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Rimonabant (SR141716) Cannabinoid Receptor antagoniste

Name: Rimonabant (SR141716)
Brand: Selleck Chemicals
SKU: S3021
Rating: 5 (8 reviews)

N° Cat.S3021

Rimonabant (SR141716) est un antagoniste sélectif de CB1 avec une IC50 de 13,6 nM et une EC50 de 17,3 nM dans la membrane de cellules HEK 293 transfectées hCB1, et c'est aussi un double inhibiteur des acyl CoA:cholesterol acyltransferases (ACAT) 1 et 2 qui inhibe le MmpL3 mycobactérien.

Rimonabant (SR141716) Cannabinoid Receptor antagoniste Chemical Structure

Structure chimique

Poids moléculaire: 463.79

Aller à

Contrôle qualité

Lot : Pureté : 99.67%

99.67

Cibles apparentées	CXCR Hedgehog/Smoothened PKA Adrenergic Receptor AChR 5-HT Receptor Histamine Receptor Dopamine Receptor Ras KRas
Autre Cannabinoid Receptor Inhibiteurs	AM1241 AM251 BML-190 Otenabant (CP-945598) HCl 6-Iodopravadoline (AM630) Org 27569 GW842166X CID16020046 WIN 55, 212-2 mesylate Yangonin

Culture cellulaire, traitement et concentration de travail

Lignées cellulaires	Type dessai	Concentration	Temps dincubation	Description de lactivité	PMID
CHO cells	Function assay			Ability to displace [3H]-SR- 141716A binding to human CB1 receptor expressed in CHO cell membranes, Ki=8.9 nM	10465552
CHO	Function assay			Antagonistic activity towards cannabinoid receptor 1 expressed as [3H]Arachidonic acid release in CHO cells, Kd=0.002512μM	14736243
CHO	Function assay			Displacement of CP-55940 binding from recombinant human cannabinoid receptor 1 expressed in CHO cells, Ki=0.025μM	14736243
CHO	Function assay			Affinity to displace CP-55940 binding from Cannabinoid receptor 2 of human expressed in CHO cells, Ki=1.58μM	14736243
CHO	Function assay			Inhibitory concentration against human recombinant cannabinoid receptor type 1 expressed in Chinese Hamster Ovary (CHO) cells, IC50=0.006μM	15713403
CHO	Function assay			In vitro cannabinoid receptor 1 antagonism of [3H]arachidonic acid release by CHO cells, Kd=0.002512μM	15771428
CHO	Function assay			In vitro displacement of CP-55940 binding to human CB1 receptor expressed in CHO cells, Ki=0.025μM	15771428
CHO	Function assay			In vitro displacement of CP-55940 binding to human CB2 receptor expressed in CHO cells, Ki=1.58μM	15771428
CHO	Function assay			Inhibition of [3H]SR-141,716A binding to human CB1 receptor expressed in CHO cells, Ki=0.0054μM	15801840
CHO	Function assay			Antagonistic activity against cannabinoid receptor 1 measured by CP-55940 induced arachnoid acid release in CHO cells, Kd=0.002512μM	16140010
CHO	Function assay			Displacement of specific CP-55940 binding in CHO cells stably transfected with human cannabinoid receptor 1, Ki=0.025μM	16140010
CHO	Function assay			Displacement of specific CP-55940 binding in CHO cells stably transfected with human cannabinoid receptor 2, Ki=1.58μM	16140010
CHOK1	Function assay			Functional activity at human CB1 receptor transfected in CHOK1 cells by [35SGTP]gammaS assay, Ki=0.001μM	16263283
HEK293	Function assay			Displacement of [3H]SR-141716 from human CB1 receptor transfected in HEK293 cells, Ki=0.0021μM	16263283
CHO	Function assay			Displacement of [3H]SR141716A from human CB1 receptor expressed in CHO cells, Ki=0.0054μM	16279809
HEK293	Function assay			Displacement of [3H]SR-141716 from human CB1 receptor expressed in HEK293 cells, Kd=0.0018μM	17004712
HEK293	Function assay			Displacement of [3H]CP-55940 from human CB1 receptor expressed in HEK293 cells, Ki=0.0071μM	17004712
HEK293	Function assay			Displacement of [3H]WIN-55212-2 from human CB1 receptor expressed in HEK293 cells, Ki=0.018μM	17004712
CHO	Function assay			Inhibition of [3H]CP-55940 binding to human recombinant CB1 receptor in CHO cells, IC50=0.0061μM	17181138
CHO	Function assay			Inhibition of [3H]CP-55940 binding to human recombinant CB2 receptor in CHO cells, IC50=0.6μM	17181138
CHO	Function assay			Displacement of [3H]CP-55940 from human recombinant CB1 receptor expressed in CHO cells, IC50=0.0061μM	17293109
CHO	Function assay			Displacement of [3H]CP-55940 from human recombinant CB2 receptor expressed in CHO cells, IC50=0.6033μM	17293109
HEK293	Function assay			Displacement of [3H]CP-559440 from human CB1 receptor expressed in HEK293 cells, Ki=0.0011μM	17383180
HEK293	Function assay			Displacement of [3H]CP-55940 from human recombinant CB1 receptor expressed in HEK293 cells, Ki=0.016μM	17942307
HEK293	Function assay			Displacement of [3H]CP-55940 from human recombinant CB2 receptor expressed in HEK293 cells, Ki=1.64μM	17942307
HEK293	Function assay			Displacement of [3H]CP-55940 from human recombinant CB1 receptor expressed in HEK293 cells, Ki=0.047μM	17979261
CHOK1	Function assay			Displacement of [3H]WIN-552122 from human recombinant CB2 receptor expressed in CHOK1 cells, Ki=1.99μM	17979261
HEK293	Function assay			Displacement of radioligand from human CB1 receptor expressed in HEK293 cells, Ki=0.0018μM	18083560
HEK293 EBNA	Function assay			Inverse agonist activity at human CB1 receptor expressed in HEK293 EBNA cells by [35S]GTPgammaS incorporation assay, EC50=0.004μM	18083560
HEK293	Function assay			Displacement of radioligand from human CB2 receptor expressed in HEK293 cells, Ki=0.554μM	18083560
CHOK1	Function assay			Antagonist activity at human CB1 receptor expressed in CHOK1 cells by luciferase assay, IC50=0.12μM	18243711
CHOK1	Function assay			Displacement of [3H]WIN-55212-2 from human CB2 receptor expressed in CHOK1 cells, IC50=1.76μM	18243711
HEK	Function assay			Displacement of [3H]CP-55940 from human recombinant CB1 receptor expressed in HEK cells, Ki=0.012μM	18293908
HEK	Function assay			Displacement of [3H]CP-55940 from human recombinant CB2 receptor expressed in HEK cells, Ki=0.79μM	18293908
HEK293	Function assay			Displacement of [3H]CP-55940 from human CB1R expressed in HEK293 cells, Ki=0.006μM	18335976
CHO	Function assay			Displacement of [3H]WIN-55212-2 from human cannabinoid CB2 receptor expressed in CHO cells, IC50=1.76μM	18337096
CHO	Function assay			Displacement of [3H]CP-55940 from human CB1 receptor expressed in CHO cells, Ki=0.025μM	18342403
CHO	Function assay			Displacement of [3H]WIN-55212-2 from human CB2 receptor expressed in CHO cells, Ki=1.58μM	18342403
HEK293	Function assay			Displacement of [3H]CP-55940 from human CB1 receptor expressed in HEK293 cells, Ki=0.0024μM	18363352
CHO	Function assay			Displacement of [3H]CP-55940 from human CB2 receptor expressed in CHO cells, Ki=0.56μM	18363352
SF9	Function assay			Antagonist activity at rat CB1 receptor in SF9 cells assessed as inhibition of CP-55940-stimulated GTPgammaS binding, Ki=0.00031μM	18448340
SF9	Function assay			Antagonist activity at human CB1 receptor expressed in SF9 cells assessed as inhibition of CP-55940-stimulated GTPgammaS binding, Ki=0.00043μM	18448340
SF9	Function assay			Inverse agonist at human CB1 receptor expressed in SF9 cells assessed as decrease in GTPgammaS level, IC50=0.00135μM	18448340
SF9	Function assay			Antagonist activity at human CB2 receptor in SF9 cells assessed as inhibition of CP-55940-stimulated GTPgammaS binding, Ki=0.815μM	18448340
HEK293	Function assay			Displacement of [3H]CP-55940 form human recombinant CB1 receptor expressed in HEK293 cells by liquid scintillation counting, Ki=0.04μM	18511157
CHO-K1	Function assay			Displacement of [3H]SR141716 from human CB1 receptor expressed in CHO-K1 cells, Ki=0.00118μM	18512901
HEK293	Function assay			Antagonist activity at human CB1 receptor expressed in HEK293 cells assessed as inhibition of CP-55940-stimulated [35S]GTPgammaS binding, Kd=0.00257μM	18512901
HEK293	Function assay			Displacement of [3H]CP-55940 from human CB1 receptor expressed in HEK293 cells, Ki=0.00618μM	18512901
CHO-K1	Function assay			Displacement of [3H]CP-55940 from human CB2 receptor expressed in CHO-K1 cells, Ki=0.313μM	18512901
HEK	Function assay			Displacement of [3H]CP-55940 from human recombinant CB1 receptor expressed in HEK cells, Ki=0.008μM	18579386
HEK	Function assay			Displacement of [3H]CP-55940 from human recombinant CB2 receptor expressed in HEK cells, Ki=0.79μM	18579386
HEK293	Function assay			Displacement of [3H]CP-55940 from human CB1 receptor expressed in HEK293 cells, Ki=0.012μM	18680276
HEK293	Function assay			Displacement of [3H]CP-55940 from human CB2 receptor expressed in HEK293 cells, Ki=0.79μM	18680276
HEK293	Function assay			Displacement of [3H]CP-55940 from human CB1 receptor expressed in HEK293 cells, IC50=0.015μM	18712856
HEK293	Function assay			Antagonist activity at human CB1 receptor expressed in HEK293 cells assessed as inhibition of Eu-GTP binding, EC50=0.0182μM	18712856
HEK293	Function assay			Displacement of [3H]CP-55940 from human CB2 receptor expressed in HEK293 cells, IC50=1.9398μM	18712856
HEK293	Function assay			Inverse agonist activity at human CB1 receptor expressed in HEK293 cells assessed as decrease in [35S]gammaGTP binding relative to control	18712856
CHO	Function assay			Antagonist activity at human CB1 receptor in CHO cells assessed as GTPgammaS binding, Kb=0.000698μM	18800770
CHOK1	Function assay			Displacement of [3H]WIN-55212-2 from human CB2 receptor expressed in CHOK1 cells by liquid scintillation spectrometry, IC50=1.76μM	18954042
CHO	Function assay			Displacement of [3H]WIN-55212-2 from human CB2 receptor expressed in CHO cells, IC50=1.76μM	19022666
HEK293	Function assay			Displacement of [3H]CP-55940 from human CB2 receptor expressed in HEK293 cells, IC50=0.0019μM	19095444
HEK293	Function assay			Displacement of [3H]CP-55940 from human CB1 receptor expressed in HEK293 cells, IC50=0.015μM	19095444
HEK293	Function assay			Antagonist activity at human CB1 receptor expressed in HEK293 cells assessed as inhibition of Eu-GTP binding, EC50=0.0182μM	19095444
CHO-K1	Function assay			Antagonist activity against human CB1 receptor expressed in CHO-K1 cells by [35S]GTPgamma binding assay, Ki=0.00019μM	19102698
HEK293	Function assay			Displacement of [3H]SR141716A from human CB1 receptor expressed in HEK293 cells, Ki=0.0009μM	19102698
CHOK1	Function assay			Displacement of [3H]WIN-55212-2 from human recombinant cannabinoid CB2 receptor expressed in CHOK1 cells by liquid scintillation spectrometry, IC50=1.76μM	19269817
CHOK1	Function assay			Antagonist activity at human cannabinoid CB1 receptor expressed in CHOK1 cells assessed as cAMP activity, EC50=0.24μM	19328683
CHOK1	Function assay			Antagonist activity at human cannabinoid CB2 receptor expressed in CHOK1 cells assessed as cAMP activity, EC50=31.21μM	19328683
HEK293	Function assay			Displacement of [3H]SR141716 from human recombinant CB1 receptor expressed in HEK293 cells, Ki=0.001995μM	19338356
HEK293	Function assay			Displacement of [3H]SR141716 from human recombinant CB2 receptor expressed in HEK293 cells, Ki=0.39811μM	19338356
CHOK1	Function assay		10 mins	Antagonist activity at human CB1 receptor expressed in CHOK1 cells assessed as inhibition of CP-55940-induced response after 10 mins by GTPgamma[35S] binding assay, Ki=0.0016μM	19351113
HEK293	Function assay			Displacement of [3H]rimonabant from human CB1 receptor expressed in HEK293 cells by liquid scintillation counting, Ki=0.0019μM	19520572
HEK293	Function assay			Displacement of [3H]CP-55940 from human recombinant CB1R expressed in HEK293 cells, IC50=0.0132μM	19530697
HEK293	Function assay			Inverse agonist activity at human recombinant CB1R expressed in HEK293 cells assessed as inhibition of CP-55940-stimulated Eu-GTP binding, EC50=0.0157μM	19530697
HEK293	Function assay			Displacement of [3H]CP-55940 from human recombinant CB2R expressed in HEK293 cells, IC50=1.6311μM	19530697
HEK293	Function assay	10 uM		Intrinsic activity at human recombinant CB1R expressed in HEK293 cells assessed as Eu-GTP binding at 10 uM relative to basal level	19530697
HEK	Function assay			Displacement of [3H]CP-55940 from human recombinant CB1 receptor expressed in HEK cells, Ki=0.012μM	19595596
HEK	Function assay			Displacement of [3H]CP-55940 from human recombinant CB2 receptor expressed in HEK cells, Ki=0.79μM	19595596
CHO-K1	Function assay			Antagonist activity at human CB1 receptor transfected in CHO-K1cells by GTPgamma[35S] binding assay, Ki=0.0016μM	19683918
CHO	Function assay			Binding affinity to human CB2 receptor expressed in CHO cells by luciferase reporter gene assay, IC50=0.0925μM	19850473
CHOK1	Function assay			Displacement of [3H]WIN-552122 from human CB2 receptor expressed in CHOK1 cells, IC50=1.76μM	19850473
CHO-K1	Function assay			Antagonist activity at human recombinant CB1 receptor expressed in CHO-K1 cells assessed as inhibition of CP-55940-stimulated GTPgammaS binding, IC50=0.0045μM	19954978
CHO-K1	Function assay			Inverse agonist activity at human CB1 receptor expressed in CHO-K1 cells by GTPgammaS binding assay, IC50=0.0029μM	20015647
CHO-K1	Function assay			Antagonist activity at human CB1 receptor expressed in CHO-K1 cells assessed as inhibition of CP-55940-induced GTPgammaS binding, IC50=0.0045μM	20015647
COS7	Function assay			Displacement of [3H]CP-55940 from human CB1 receptor expressed in COS7 cells, IC50=0.0051μM	20015647
CHO	Function assay			Inverse agonist activity at human recombinant CB1 receptor expressed in CHO cells by luciferase reporter gene assay, IC50=0.108μM	20045337
CHO	Function assay		60 mins	Inverse agonist activity at human cannabinoid CB1 receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulation after 60 mins, EC50=0.00011μM	20047779
CHO	Function assay		3 hrs	Displacement of [3H]CP-55940 from human recombinant cannabinoid CB1 receptor expressed in CHO cells after 3 hrs by liquid scintillation counting, Ki=0.00074μM	20047779
CHO	Function assay		10 mins	Antagonist activity at human cannabinoid CB1 receptor expressed in CHO cells coexpressing Galpha15/16 assessed as inhibition of CP-55940-induced Ca2+ release after 10 mins by micro plate reader, IC50=0.0032μM	20047779
CHO	Function assay		3 hrs	Displacement of [3H]CP-55940 from human recombinant cannabinoid CB2 receptor expressed in CHO cells after 3 hrs by liquid scintillation counting, Ki=0.126μM	20047779
CHO	Function assay			Antagonist activity at human CB1 receptor expressed in CHO cells assessed as inhibition of CP-55940-induced [3H]arachidonic acid release, Kd=0.002512μM	20363132
CHO	Function assay			Displacement of [3H]CP-55940 from human CB1 receptor expressed in CHO cells, Ki=0.025μM	20363132
CHO	Function assay			Displacement of [3H]CP-55940 from human CB2 receptor expressed in CHO cells, Ki=1.58μM	20363132
CHO-K1	Function assay		1 hr	Displacement of [3H]WIN-55212-2 from human CB2 receptor expressed in CHO-K1 cells after 1 hr by liquid scintillation counting, IC50=1.76μM	20673729
HEK	Function assay			Displacement of [3H]CP-55940 from human CB1 receptor expressed in HEK cells, Ki=0.012μM	20718492
HEK	Function assay			Displacement of [3H]CP-55940 from human CB2 receptor expressed in HEK cells, Ki=0.79μM	20718492
CHO	Function assay			Agonist activity at human CB1 receptor expressed in CHO cells co-expressing Galpha16 protein assessed as mobilization of intracellular calcium, Ke=0.0011μM	20845959
HEK293	Function assay			Displacement of [3H]SR141716 from human CB1 receptor expressed in HEK293 cells, Ki=0.00118μM	20845959
HEK293	Function assay			Displacement of [3H]CP55940 from human CB1 receptor expressed in HEK293 cells, Ki=0.00618μM	20845959
CHOK1	Function assay			Displacement of [3H]CP55940 from human CB2 receptor expressed in CHOK1 cells, Ki=0.313μM	20845959
HEK	Function assay			Displacement of [3H]CP-55,940 from recombinant human CB1 receptor transfected in HEK cells, Ki=0.012μM	20943290
HEK	Function assay			Displacement of [3H]CP-55,940 from recombinant human CB2 receptor transfected in HEK cells, Ki=0.79μM	20943290
CHO	Function assay			Displacement of [3H]SR141716A from human CB1 receptor expressed in CHO cells, Ki=0.0009333μM	21334892
Sf9	Function assay			Displacement of [3H]CP55940 from human recombinant CB2 receptor expressed in Sf9 cells, Ki=0.85114μM	21334892
CHO	Function assay			Antagonist activity at CB1 receptor transfected in CHO cells expressing apoaequorin as a reporter for G-protein-coupled receptor-mediated calcium signaling by bioluminescence assay, IC50=0.004μM	21376588
HEK293	Function assay			Noncompetitive inhibition of MRP1-mediated E2-17betaG transport in human MRP1 expressing HEK293 cells by Dixon plot, Ki=1.4μM	21511945
HEK293	Function assay			Noncompetitive inhibition of MRP4-mediated E2-17betaG transport in human MRP4 expressing HEK293 cells by Dixon plot, Ki=4μM	21511945
HEK293	Function assay			Induction of MRP2-mediated E2-17betaG transport in human MRP2 expressing HEK293 cells in presence of 2 uM E2-17betaG	21511945
HEK293	Function assay			Inhibition of MRP3-mediated E2-17betaG transport in human MRP3 expressing HEK293 cells in presence of 15 uM E2-17betaG	21511945
HEK293	Function assay			Inhibition of MRP1-mediated E2-17betaG transport in human MRP1 expressing HEK293 cells in presence of 0.6 to 5 uM E2-17betaG	21511945
HEK293	Function assay			Inhibition of MRP4-mediated E2-17betaG transport in human MRP4 expressing HEK293 cells in presence of 0.6 to 5 uM E2-17betaG	21511945
HEK	Function assay			Displacement of [3H]CP-55940 from human recombinant CB1 receptor expressed in HEK cells, Ki=0.012μM	21702498
HEK	Function assay			Displacement of [3H]CP-55940 from human recombinant CB2 receptor expressed in HEK cells, Ki=0.79μM	21702498
CHO	Function assay		1 hr	Displacement of [3H]CP55940 from human cannabinoid CB2 receptor expressed in CHO cells at pH 7.4 after 1 hr by liquid scintillation counting, IC50=1.98μM	21741835
HEK293	Function assay		5 mins	Inhibition of human ERG expressed in HEK293 cells assessed as inhibition of potassium channel current after 5 mins by patch clamp assay, IC50=2.79μM	21741835
CHO	Function assay		90 mins	Displacement of [3H]BMS-725519 from human CB1 receptor expressed in CHO cells after 90 mins by scintillation counting, Ki=0.00073μM	21962575
CHO-K1	Function assay			Antagonist activity at human CB1 receptor expressed in CHO-K1 cells co-expressing Galphaq16 assessed as inhibition of CP55940-induced intracellular calcium mobilization by fluorometry, Ke=0.0011μM	22372835
CHO-K1	Function assay			Displacement of [3H]CP55940 from human CB1 receptor expressed in CHO-K1 cells, Ki=0.0062μM	22372835
CHO-K1	Function assay			Displacement of [3H]CP55940 from CB2 receptor expressed in CHO-K1 cells, Ki=0.313μM	22372835
HEK	Function assay			Displacement of [3H]CP-55,940 from human recombinant CB1 receptor transfected in HEK cells, Ki=0.012μM	22548457
HEK	Function assay			Displacement of [3H]CP-55,940 from human recombinant CB2 receptor transfected in HEK cells, Ki=0.79μM	22548457
CHO	Function assay		2 hrs	Displacement of [3H]CP55,940 from human CB1 receptor expressed in CHO cells after 2 hrs by liquid scintillation counter, Ki=0.0126μM	22916707
CHO	Function assay		2 hrs	Displacement of [3H]CP55,940 from human CB2 receptor expressed in CHO cells after 2 hrs by liquid scintillation counter, Ki=0.9μM	22916707
CHO	Function assay			Inverse agonist activity against CB1 receptor expressed in human CHO cells assessed as effect on forskolin-stimulated cAMP level, IC50=0.051μM	22959249
CHO	Function assay		1 hr	Displacement of [3H]CP55940 from human CB1 receptor expressed in CHO cells incubated for 1 hr, Ki=0.0106μM	23072339
CHO	Function assay	> 0.1 nM	1 hr	Inverse agonist activity at human recombinant CB1 receptor transfected in CHO cells assessed as reduction of [35S]GTPgammaS binding at > 0.1 nM after 1 hr by liquid scintillation spectrometry	23357307
N1E-115	Function assay	1 uM	5 mins	Inverse agonist activity at CB1 receptor in mouse N1E-115 cells assessed as inhibition of WIN 55,212-2-induced ERK1/2 phosphorylation at 1 uM treated 5 mins prior to WIN 55,212-2 challenge by Western blot analysis	23357307
CHO	Function assay			Antagonist activity at human GPR18 transfected in CHO cells assessed as delta9-THC-induced beta-arrestin recruitment incubated 60 mins prior to delta9-THC addition by beta-arrestin translocation assay, IC50=10.1μM	23679955
HEK	Function assay		1 hr	Antagonist activity at human CB1 receptor overexpressed in HEK cells assessed as [35S]GTPgamma binding after 1 hr by liquid scintillation counting analysis, EC50=0.0015μM	24175572
CHOK1	Function assay		1 hr	Displacement of [3H]CP55940 from human CB1 receptor expressed in CHOK1 cells after 1 hr by liquid scintillation counting analysis, Ki=0.0059μM	24175572
CHO	Function assay		45 mins	Antagonist activity at human CB1 receptor stably expressed in CHO cells co-expressing co-expressing Ga15/16 assessed as calcium current after 45 mins by fluo-4 AM assay, IC50=0.013μM	24445310
CHO	Function assay		45 mins	Antagonist activity at CB2 receptor (unknown origin) stably expressed in CHO cells co-expressing co-expressing Ga15/16 assessed as calcium current after 45 mins by fluo-4 AM assay, IC50=9.8μM	24445310
CHO-K1	Function assay		10 mins	Antagonist activity at human CB1 receptor expressed in CHO-K1 cells assessed as inhibition of CP-55940-induced [35S]GTPgammaS binding incubated for 10 mins prior to CP-55940-challenge measured after 1 hr by beta counting, Ki=0.0016μM	24900484
HEK293	Function assay		60 mins	Displacement of [3H]SR141716A form human CB1 receptor expressed in HEK293 cells after 60 mins by beta counting, Ki=0.0018μM	24900484
CHO-K1	Function assay		60 mins	Displacement of [3H]CP-55940 from human CB2 receptor expressed in CHO-K1 cells after 60 mins by beta counting, Ki=0.522μM	24900484
CHO	Function assay		2 hrs	Displacement of [3H]CP55,940 from recombinant human CB1 receptor expressed in CHO cells after 2 hrs by liquid scintillation counting, Ki=0.0126μM	24900561
CHO	Function assay		2 hrs	Displacement of [3H]CP55,940 from recombinant human CB2 receptor expressed in CHO cells after 2 hrs by liquid scintillation counting, Ki=0.9μM	24900561
CHO	Function assay		90 mins	Agonist activity at GPR55 (unknown origin) expressed in CHO cells assessed as inhibition of LPI-induced beta-arrestin translocation after 90 mins by luminescence assay, EC50=2.01μM	24900561
RD-HGA16	Function assay			Antagonist activity at CB1-OX1 heterodimer (unknown origin) expressed in RD-HGA16 cells assessed as inhibition of orexin A-induced calcium mobilization by fluorometric imaging plate reader analysis, Ke=0.001μM	24944734
RD-HGA16	Function assay			Antagonist activity at CB1 receptor (unknown origin) expressed in RD-HGA16 cells assessed as inhibition of CP55940-induced calcium mobilization by fluorometric imaging plate reader analysis, Ke=0.0011μM	24944734
Sf9	Function assay		20 mins	Inverse agonist activity at human CB1 receptor expressed in Sf9 cells coexpressing Gbeta1gamma2 and RSG4 assessed as degradation of [gamma-33P]GTP after 20 mins by steady-state GTPase assay, EC50=0.05μM	25096297
Sf9	Function assay		20 mins	Inverse agonist activity at human CB1 receptor expressed in Sf9 cells coexpressing Gbeta1gamma2 and RSG4 assessed as degradation of [gamma-33P]GTP after 20 mins by steady-state GTPase assay, EC50=0.05012μM	25096297
CHO	Function assay			Antagonist activity against CB1R (unknown origin) CHO cells stably expressing Galpha16 assessed as inhibition of CP55940-induced increase in intracellular calcium level pre-treated 10 mins before CP55940 stimulation by microplate reader based assay, IC50=0.0135μM	26151231
CHO	Function assay			Antagonist activity against CB2R (unknown origin) CHO cells stably expressing Galpha16 assessed as inhibition of CP55940-induced increase in intracellular calcium level pre-treated 10 mins before CP55940 stimulation by microplate reader based assay, IC50=9.1μM	26151231
HEK293	Function assay			Immediate antagonist/Inverse agonist activity at hemagglutinin-tagged human CB1 receptor expressed in HEK293 cells assessed as reversal of 1 uM CP55,940-induced inhibition of 5 uM forskolin-induced cAMP accumulation by kinetic cAMP assay	26203658
HEK293	Function assay		90 mins	Displacement of [3H]-CP-55940 from human recombinant CB1 receptor expressed in HEK293 cells after 90 mins by Competition binding assay, Kieq=0.012μM	26756097
HEK293	Function assay		90 mins	Displacement of [3H]-CP-55940 from human recombinant CB2 receptor expressed in HEK293 cells after 90 mins by Competition binding assay, Kieq=0.79μM	26756097
CHO-K1	Function assay			Antagonist activity at human CB1 receptor expressed in CHO-K1 cells assessed as inhibition of CP55940-induced intracellular calcium mobilization by Calcein-4 AM-staining based FLIPR assay, Ke=0.0011μM	26827137
CHO	Function assay		90 secs	Inverse agonist activity at human CB1 receptor expressed in CHO cells assessed as increase in intracellular calcium mobilization after 90 secs by Calcein-4 AM-staining based FLIPR assay, EC50=0.005μM	26827137
SJ-GBM2	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SJ-GBM2 cells	29435139
A673	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for A673 cells	29435139
SK-N-MC	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-MC cells	29435139
BT-37	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-37 cells	29435139
SK-N-SH	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-SH cells	29435139
NB1643	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB1643 cells	29435139
LAN-5	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for LAN-5 cells	29435139
BT-12	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-12 cells	29435139
OHS-50	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for OHS-50 cells	29435139
RD	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for RD cells	29435139
A673	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for A673 cells)	29435139
SK-N-MC	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for SK-N-MC cells	29435139
DAOY	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for DAOY cells	29435139
TC32	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for TC32 cells	29435139
U-2 OS	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for U-2 OS cells	29435139
Rh41	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for Rh41 cells	29435139
Saos-2	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for Saos-2 cells	29435139
CHOK1	Function assay		90 mins	Inverse agonist activity at C-terminally prolink-tagged mouse CB2 receptor expressed in CHOK1 cells harboring beta-galactosidase enzyme fused beta-arrestin assessed as increase in beta-arrestin recruitment after 90 mins by chemiluminescent assay, EC50=0.015μM	29939744
HEK293	Function assay			Antagonist activity at human CB1 receptor expressed in HEK293 cells by GTPgammaS binding assay, Ke=0.0002μM	30077609
HEK293	Function assay		90 secs	Inverse agonist activity at human CB1 receptor expressed in HEK293 cells co-expressing Galphaq16 assessed as inhibition of calcium mobilization after 90 secs by calcein-4 AAM dye-based FLIPR assay, EC50=0.586μM	30077609
HEK293	Function assay		30 mins	Inverse agonist activity at human CB1 receptor expressed in HEK293 cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins by HTRF assay, EC50=0.0041μM	30339387
CHO	Function assay			Displacement of [3H]-CP55940 from human recombinant cannabinoid CB1 receptor expressed in CHO cells by radioligand binding assay, Ki=0.143μM	31609608
CHO	Function assay			Agonist activity at human GPR55 expressed in CHO cells assessed as induction of LPI-induced beta-arrestin recruitment by beta-galactosidase enzyme fragment complementation method, EC50=2.01μM	ChEMBL
CHO	Function assay			Agonist activity at human GPR18 expressed in CHO cells assessed as induction of beta-arrestin recruitment by beta-galactosidase enzyme fragment complementation method, EC50=10.1μM	ChEMBL
Cliquez pour voir plus de données expérimentales sur les lignées cellulaires

Informations chimiques, stockage et stabilité

Poids moléculaire	463.79	Formule	C₂₂H₂₁Cl₃N₄O	Stockage (À partir de la date de réception)	3 ans-20°Cpoudre
N° CAS	168273-06-1	Télécharger le SDF		Stockage des solutions mères	1 an-80°Cen solvant 1 mois-20°Cen solvant
Synonymes	N/A			Smiles	CC1=C(N(N=C1C(=O)NN2CCCCC2)C3=C(C=C(C=C3)Cl)Cl)C4=CC=C(C=C4)Cl

Solubilité

In vitro
Lot:

DMSO : 92 mg/mL (198.36 mM)
(Le DMSO contaminé par lhumidité peut réduire la solubilité. Utiliser du DMSO frais et anhydre.)

Ethanol : 50 mg/mL

Water : Insoluble

Calculateur de molarité

Masse	Concentration	Volume	Poids moléculaire
=	×	×

Calculateur de dilution Calculateur de poids moléculaire

In vivo Lot:
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Clear solution	5%DMSO 1 40%PEG300 2 5%Tween80 3 ddH2O Validé par les laboratoires Selleck. Si vous avez besoin dajustements à cette formulation, contactez notre équipe de vente pour des tests personnalisés.	5.000mg/ml (10.78mM)	Taking the 1 mL working solution as an example, add 50 μL of 100 mg/ml clarified DMSO stock solution to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to make it clear; then continue to add 500 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.

Calculateur de formulation in vivo (Solution claire)

Étape 1 : Entrez les informations ci-dessous (Recommandé : Un animal supplémentaire pour tenir compte des pertes pendant lexpérience)

Dosage : mg/kg Poids moyen des animaux : g Volume de dosage par animal :μL Nombre danimaux :

Étape 2 : Entrez la formulation in vivo (Ceci nest que le calculateur, pas la formulation. Veuillez nous contacter dabord sil ny a pas de formulation in vivo dans la section Solubilité.)

% DMSO + % + % Tween 80 + % ddH₂O

%DMSO+ %

Résultats du calcul :

Concentration de travail : mg/ml;

Méthode de préparation du liquide maître DMSO : mg médicament prédissous dans μL DMSO ( Concentration du liquide maître mg/mL, Veuillez nous contacter dabord si la concentration dépasse la solubilité du DMSO du lot de médicament. )

Méthode de préparation de la formulation in vivo : Prendre μL DMSO liquide maître, ajouter ensuiteμL PEG300, mélanger et clarifier, ajouter ensuiteμL Tween 80, mélanger et clarifier, ajouter ensuite μL ddH₂O, mélanger et clarifier.

Méthode de préparation de la formulation in vivo : Prendre μL DMSO liquide maître, ajouter ensuite μL Huile de maïs, mélanger et clarifier.

Remarque : 1. Assurez-vous que le liquide est clair avant dajouter le solvant suivant.
2. Assurez-vous dajouter le(s) solvant(s) dans lordre. Vous devez vous assurer que la solution obtenue lors de lajout précédent est une solution claire avant de procéder à lajout du solvant suivant. Des méthodes physiques telles que le vortex, les ultrasons ou le bain-marie peuvent être utilisées pour faciliter la dissolution.

Mécanisme daction

Fonctionnalités	Efficacious to induce weight reduction and improvements in cardiometabolic risk factors, however was withdrawn in 2009 due to severe depressive disorder and anxiety.
Targets/IC₅₀/Ki	ACAT1 ACAT2 MmpL3 hCB1 (Cell-free assay) 13.6 nM hCB2 (Cell-free assay) 1.64 μM
In vitro	Rimonabant (SR141716) réduit l'activité ACAT de manière dose-dépendante dans les macrophages Raw264.7 avec une IC50 de 2,9 μM et les macrophages péritonéaux isolés. Il inhibe l'activité ACAT dans les cellules CHO-ACAT1 et CHO-ACAT2 intactes et dans des tests sans cellules avec une efficacité approximativement égale, avec une IC50 de 1,5 μM et 2,2 μM pour CHO-ACAT1 et CHO-ACAT2, respectivement. Conformément à l'inhibition d'ACAT, le traitement par ce composé bloque les processus dépendants d'ACAT dans les macrophages, l'apoptose induite par l'oxystérol et la formation de cellules spumeuses induite par le LDL acétylé. Il antagonise les effets inhibiteurs des agonistes des Cannabinoid Receptor sur les contractions du canal déférent de la souris et sur l'activité de l'adénylyl cyclase dans les membranes cérébrales de rat de manière concentration-dépendante. Le composé réduit significativement la croissance cellulaire et induit la mort cellulaire des cellules cancéreuses colorectales humaines (DLD-1, CaCo-2 et SW620). Il est capable de modifier la distribution du cycle cellulaire dans toutes les lignées cellulaires testées. En particulier, Rimonabant produit un arrêt du cycle cellulaire en phase G2/M dans les cellules DLD-1 sans induire d'apoptose ou de nécrose.
Kinase Assay	Essai de liaison au radioligand
Kinase Assay	Les cellules HEK 293 transfectées de manière stable avec les récepteurs CB1 et CB2 humains sont purifiées. 0,2-8 μg de la membrane purifiée sont incubés avec 0,75 nM de [³H] CP55,940 et Rimonabant (SR141716) dans le tampon d'incubation (50 mM Tris-HCl, 5 mM MgCl₂, 1 mM EDTA, 0,3% BSA, pH 7,4). La liaison non spécifique est définie en présence de 1 μM de CP55,940. Les réactions sont incubées pendant une heure et demie à 30 °C dans Multiscreen. Les réactions sont terminées par filtration multiple et lavées quatre fois avec un tampon de lavage glacé (50 mM Tris, pH 7,4, 0,25% BSA). La radioactivité liée aux filtres est mesurée par Topcount. L'IC50 est déterminée comme la concentration de ce composé requise pour inhiber 50% de la liaison de [³H] CP55,940 et calculée par régression non linéaire.
In vivo	Rimonabant (SR141716) est administré par voie intrapéritonéale ou orale et antagonise puissamment et de manière dose-dépendante les effets pharmacologiques et comportementaux classiques des agonistes des Cannabinoid Receptor. Dans le modèle murin de carcinogenèse colique induite par l'azoxyméthane, il a significativement diminué la formation de foyers cryptiques aberrants (FCA), qui précède le cancer colorectal. Ce composé (10 mg/kg par gavage) est administré pendant 2 semaines à des rats Zucker mâles obèses de 3 mois comme modèle d'intolérance au glucose et pendant 10 semaines à des rats Zucker mâles obèses de 6 mois comme modèle de syndrome métabolique. Les niveaux sériques de RANTES (Regulated upon Activation, Normal T cell Expressed, and Secreted) et de MCP-1 (monocyte chemotactic protein-1) sont augmentés chez les rats Zucker obèses par rapport aux rats maigres et significativement réduits par un traitement à long terme avec celui-ci, ce qui ralentit la prise de poids chez les rats atteints du syndrome métabolique. Les neutrophiles et les monocytes sont significativement augmentés chez les jeunes et vieux rats Zucker obèses par rapport aux rats maigres et diminués par ce composé. Le fibrinogène lié aux plaquettes est significativement augmenté chez les rats Zucker obèses par rapport aux rats maigres des deux âges, et est réduit par celui-ci. Les plaquettes des rats obèses sont plus sensibles à l'agrégation induite par la thrombine et à l'adhésion au fibrinogène, qui sont toutes deux atténuées par la thérapie au Rimonabant.
Références	[1] https://pubmed.ncbi.nlm.nih.gov/18802648/ [2] https://pubmed.ncbi.nlm.nih.gov/20609360/ [3] https://pubmed.ncbi.nlm.nih.gov/8070571/ [4] https://pubmed.ncbi.nlm.nih.gov/19479993/ [5] https://pubmed.ncbi.nlm.nih.gov/18469848/ [6] https://pubmed.ncbi.nlm.nih.gov/17213845/ [7] https://pubmed.ncbi.nlm.nih.gov/30682372/

Applications

Méthodes	Biomarqueurs	Images	PMID
Western blot	CD44 / Lgr5 / CD133 / EpCAM β-catenin p-LRP6 / LRP6 / Lgr5		29354056
Immunofluorescence	β-catenin Lgr5		29354056

Informations sur lessai clinique

(données de https://clinicaltrials.gov, mis à jour le 2024-05-22)

Numéro NCT	Recrutement	Conditions	Sponsor/Collaborateurs	Date de début	Phases
NCT00750347	Completed	Pain	University Hospital Clermont-Ferrand	September 2008	Phase 1
NCT00656487	Completed	Cannabis Dependence\|Cannabis Withdrawal	The Scripps Research Institute\|National Institute on Drug Abuse (NIDA)	April 30 2008	Phase 2
NCT00546325	Completed	Diabetes Mellitus Type 2	Sanofi	October 2007	Phase 3
NCT00525681	Completed	Renal Transplantation	University of Oslo School of Pharmacy	September 2007	Phase 4
NCT00584389	Terminated	Obesity	University of Surrey\|European Foundation for the Study of Diabetes\|Royal Surrey County Hospital NHS Foundation Trust	July 2007	Phase 4
NCT01041170	Completed	Cannabis\|Dependence	National Institute on Drug Abuse (NIDA)\|National Institutes of Health Clinical Center (CC)	April 16 2006	Phase 1

Support technique

Instructions de manipulation

Tel: +1-832-582-8158 Ext:3

Si vous avez dautres questions, veuillez laisser un message.

C1=C0/X	C1:	LOG(C1):
C2=C1/X	C2:	LOG(C2):
C3=C2/X	C3:	LOG(C3):
C4=C3/X	C4:	LOG(C4):
C5=C4/X	C5:	LOG(C5):
C6=C5/X	C6:	LOG(C6):
C7=C6/X	C7:	LOG(C7):
C8=C7/X	C8:	LOG(C8):