nur für Forschungszwecke
Nelfinavir Mesylate HIV Protease Inhibitor
Kat.-Nr.S4282
Chemische Struktur
Molekulargewicht: 663.89
Springe zu
Qualitätskontrolle
Charge:
Reinheit:
99.51%
99.51
| Verwandte Ziele | HDAC Caspase Proteasome Secretase MMP HCV Protease Cysteine Protease DPP Tyrosinase Serine Protease |
|---|---|
| Weitere HIV Protease Inhibitoren | Pepstatin A Limonin Temsavir (BMS-626529) NBD-556 Bevirimat GS-6207 Rosamultin Dextran sulfate sodium (DSS) Mericitabine Azvudine |
Zellkultur, Behandlung & Arbeitskonzentration
| Zelllinien | Assay-Typ | Konzentration | Inkubationszeit | Formulierung | Aktivitätsbeschreibung | PMID |
|---|---|---|---|---|---|---|
| HeLa | Function assay | TP_TRANSPORTER: inhibition of TEA uptake (TEA: 10 uM) in OCT1-expressing HeLa cells, IC50=21.8μM. | 10681378 | |||
| Caco-2 | Function assay | TP_TRANSPORTER: inhibition of Daunorubicin transepithelial transport (basal to apical) (Daunorubicin: 5 uM) in Caco-2 cells, IC50=1.4μM. | 10820137 | |||
| MT-4 | Antiviral assay | Anti-HIV-1 activity against Wild type virus in MT-4 cells, ED50=0.02μM. | 11543677 | |||
| MT-4 | Antiviral assay | Anti-HIV-1 activity against mutant HIV-1 in MT-4 cells (mutation selected with compound 1), ED50=0.07μM. | 11543677 | |||
| MT-4 | Antiviral assay | Anti-HIV-1 activity against mutant HIV-1 in MT-4 cells (mutation selected with ritonavir), ED50=0.11μM. | 11543677 | |||
| MT-4 | Antiviral assay | Anti-HIV-1 activity against mutant HIV-1 in MT-4 cells (mutation selected with saquinavir), ED50=0.12μM. | 11543677 | |||
| MT-4 | Antiviral assay | Anti-HIV-1 activity against mutant HIV-1 in MT-4 cells (mutation selected with nelfinavir), ED50=2.44μM. | 11543677 | |||
| LLC-PK1 | Function assay | Inhibition of P-glycoprotein, mouse L-mdr1a expressed in LLC-PK1 epithelial cells using calcein-AM polarisation assay, IC50=2.3μM. | 12699389 | |||
| LLC-PK1 | Function assay | TP_TRANSPORTER: inhibition of Calcein-AM efflux in Mdr1a-expressing LLC-PK1 cells, IC50=2.3μM. | 12699389 | |||
| LLC-PK1 | Function assay | Inhibition of P-glycoprotein, human L-MDR1 expressed in LLC-PK1 epithelial cells using calcein-AM polarisation assay, IC50=3.4μM. | 12699389 | |||
| LLC-PK1 | Function assay | TP_TRANSPORTER: inhibition of Calcein-AM efflux in MDR1-expressing LLC-PK1 cells, IC50=3.4μM. | 12699389 | |||
| HEK | Function assay | TP_TRANSPORTER: increase in mitoxantrone intracellular accumulation in BCRP-expressing HEK cells, IC50=12.5μM. | 15007102 | |||
| CEM-SS | Antiviral assay | 6 days | Antiviral activity against HIV1 3B infected in human CEM-SS cells assessed as inhibition of virus-induced cytopathic effect after 6 days by MTS assay, ED50=0.03μM. | 15217281 | ||
| HOG.R5 | Antiviral assay | 4 days | Antiviral activity against HIV1 3B infected in human HOG.R5 cells after 4 days, IC50=0.09μM. | 15217281 | ||
| MT-4 | Function assay | Effective dose of compound required to inhibit replication of human immunodeficiency virus type 1 in MT-4 cells, ED50=0.02μM. | 15537350 | |||
| MT4 | Antiviral assay | Antiviral activity against HIV1 HXB2 in MT4 cells, IC50=0.32μM. | 16458505 | |||
| MT4 | Antiviral assay | Antiviral activity against HIV1 EP13 in MT4 cells, IC50=0.45μM. | 16458505 | |||
| PHA-PBMC | Antiviral assay | Antiviral activity against HIV1 BA-L isolate in human PHA-PBMC cells, IC50=0.007μM. | 16913714 | |||
| MT2 | Antiviral assay | Antiviral activity against HIV1 LAI isolate in human MT2 cells, IC50=0.01μM. | 16913714 | |||
| PHA-PBMC | Antiviral assay | Antiviral activity against HIV1 LAI isolate in human PHA-PBMC cells, IC50=0.014μM. | 16913714 | |||
| MT2 | Antiviral assay | Antiviral activity against HIV2 EHO isolate in human MT2 cells, IC50=0.02μM. | 16913714 | |||
| PHA-PBMC | Antiviral assay | Antiviral activity against multi drug-resistant HIV1 ET variant in human PHA-PBMC cells, IC50=0.032μM. | 16913714 | |||
| PHA-PBMC | Antiviral assay | Antiviral activity against multi drug-resistant HIV1 G variant in human PHA-PBMC cells, IC50=0.17μM. | 16913714 | |||
| PHA-PBMC | Antiviral assay | Antiviral activity against multi drug-resistant HIV1 C variant in human PHA-PBMC cells, IC50=0.31μM. | 16913714 | |||
| MT2 | Antiviral assay | Antiviral activity against HIV2 EHO in MT2 cells assessed as inhibition of p24 Gag protein expression by MTT assay, EC50=0.03μM. | 17371811 | |||
| MT2 | Antiviral assay | Antiviral activity against HIV1 LAI in MT2 cells assessed as inhibition of p24 Gag protein expression by MTT assay, EC50=0.032μM. | 17371811 | |||
| MT4 | Antiviral assay | Antiviral activity against HIV1 NL4-3 in MT4 cells by MTT assay, EC50=0.033μM. | 17371811 | |||
| MT4 | Antiviral assay | Antiviral activity against HIV1 GRL98065p20 in MT4 cells assessed as inhibition of p24 Gag protein expression by MTT assay, EC50=0.08μM. | 17371811 | |||
| MT4 | Antiviral assay | Antiviral activity against ritonavir-resistant HIV1 in MT4 cells assessed as inhibition of p24 Gag protein expression by MTT assay, EC50=0.21μM. | 17371811 | |||
| MT4 | Antiviral assay | Antiviral activity against amprenavir-resistant HIV1 in MT4 cells assessed as inhibition of p24 Gag protein expression by MTT assay, EC50=0.22μM. | 17371811 | |||
| MT2 | Antiviral assay | Antiviral activity against HIV2 ROD in MT2 cells assessed as inhibition of p24 Gag protein expression by MTT assay, EC50=0.24μM. | 17371811 | |||
| MT4 | Antiviral assay | Antiviral activity against atazanavir-resistant HIV1 in MT4 cells assessed as inhibition of p24 Gag protein expression by MTT assay, EC50=0.27μM. | 17371811 | |||
| MT4 | Antiviral assay | Antiviral activity against HIV1 GRL98065p30 in MT4 cells assessed as inhibition of p24 Gag protein expression by MTT assay, EC50=0.27μM. | 17371811 | |||
| MT4 | Antiviral assay | Antiviral activity against HIV1 GRL98065p40 in MT4 cells assessed as inhibition of p24 Gag protein expression by MTT assay, EC50=0.34μM. | 17371811 | |||
| MT4 | Antiviral assay | Antiviral activity against idinavir-resistant HIV1 in MT4 cells assessed as inhibition of p24 Gag protein expression by MTT assay, EC50=0.47μM. | 17371811 | |||
| MT4 | Antiviral assay | Antiviral activity against saquinavir-resistant HIV1 in MT4 cells assessed as inhibition of p24 Gag protein expression by MTT assay, EC50=0.48μM. | 17371811 | |||
| MT4 | Antiviral assay | Antiviral activity against lopinavir-resistant HIV1 in MT4 cells assessed as inhibition of p24 Gag protein expression by MTT assay, EC50=0.49μM. | 17371811 | |||
| MT2 | Cytotoxicity assay | Cytotoxicity against human MT2 cells assessed as inhibition of p24 Gag protein expression by MTT assay, CC50=8.1μM. | 17371811 | |||
| MT4 | Antiviral assay | Antiviral activity against HIV1 3B in MT4 cells by MTT assay, EC50=0.016μM. | 17537628 | |||
| MT4 | Cytotoxicity assay | Cytotoxicity against MT4 cells by MTT assay, LC50=11μM. | 17537628 | |||
| MT4 | Antiviral assay | 5 days | Antiviral activity against HIV1 NL4-3 infected in human MT4 cells assessed as reduction in virus-induced cytopathic effect after 5 days by MTT assay, EC50=0.018μM. | 17576848 | ||
| MT4 | Antiviral assay | 5 days | Antiviral activity against HIV2 MS infected in human MT4 cells assessed as reduction in virus-induced cytopathic effect after 5 days by MTT assay, EC50=0.048μM. | 17576848 | ||
| CEM | Antiviral assay | 7 days | Antiviral activity against HIV2 ROD with protease G17N/V47A mutation infected in human CEM cells assessed as inhibition of virus production after 7 days by Lenti-RT activity assay, EC50=0.1μM. | 17576848 | ||
| CEM | Antiviral assay | 7 days | Antiviral activity against HIV2 ROD with protease V47A mutation infected in human CEM cells assessed as inhibition of virus production after 7 days by Lenti-RT activity assay, EC50=0.177μM. | 17576848 | ||
| CEM | Antiviral assay | 7 days | Antiviral activity against HIV2 ROD with protease G17N mutation infected in human CEM cells assessed as inhibition of virus production after 7 days by Lenti-RT activity assay, EC50=0.199μM. | 17576848 | ||
| CEM | Antiviral assay | 7 days | Antiviral activity against wild type HIV2 ROD infected in human CEM cells assessed as inhibition of virus production after 7 days by Lenti-RT activity assay, EC50=0.281μM. | 17576848 | ||
| HEK293 | Antiviral assay | 48 hrs | Antiviral activity against wild type HIV1 NL4-3 in HEK293 cells after 48 hrs by replication-deffective luciferase reporter gene-based phenotypic assay, EC50=0.0058μM. | 17638694 | ||
| MT4 | Antiviral assay | 6 days | Antiviral activity against wild type HIV1 NL4-3 infected in MT4 cells after 6 days by MTT assay, EC50=0.029μM. | 17638694 | ||
| MT4 | Cytotoxicity assay | 6 days | Cytotoxicity against human MT4 cells after 6 days by MTT assay, CC50=8μM. | 17638694 | ||
| HEK293 | Function assay | 0.12 uM | Inhibition of HIV1 NL4-3 proteins incorporation into virions transfected in HEK293 cells assessed as unprocessed gp160 Env protein at 0.12 uM by Western blot | 17646410 | ||
| HEK293 | Function assay | 0.12 uM | Inhibition of HIV1 NL4-3 proteins incorporation into virions transfected in HEK293 cells assessed as aberrant Env protein at 0.12 uM by Western blot | 17646410 | ||
| MDCK2 | Inhibition of human | Inhibition of human MDR1-dependent accumulation of calcein-AM expressed in MDCK2 cells, IC50=19.9μM. | 17664327 | |||
| MDR1 | Function assay | 20 uM | Decrease in P-glycoprotein-mediated tenofovir disoproxil fumarate efflux in MDCK2 expressing human MDR1 cells at 20 uM | 17664327 | ||
| CEM-SS | Antiviral assay | 5 days | Antiviral activity against HIV1 LAI infected in human CEM-SS cells assessed as reverse transcriptase activity after 5 days by MTT assay, IC50=0.002μM. | 17950955 | ||
| MOLT-4/3B | Antiviral assay | 4 days | Antiviral activity against HIV1 3B infected in MOLT-4/3B cells assessed as inhibition of mature virus release measured after 4 days of infection by RT assay, EC50=0.029μM. | 18316521 | ||
| MT4 | Antiviral assay | Antiviral activity against HIV1 3B in human MT4 cells assessed as inhibition of viral-induced cytopathic effect by MTT method, EC50=0.016μM. | 18426195 | |||
| MT4 | Cytotoxicity assay | Cytotoxicity against human MT4 cells by MTT assay, CC50=11μM. | 18426195 | |||
| MT4 | Antiretroviral assay | Antiretroviral activity against Human immunodeficiency virus 1 NL4.3 infected in human MT4 cells assessed as inhibition of virus-induced cytopathic effect by MTT assay, EC50=0.023μM. | 18541726 | |||
| MT4 | Antiretroviral assay | Antiretroviral activity against Human immunodeficiency virus 1 3B infected in human MT4 cells assessed as inhibition of virus-induced cytopathic effect by MTT assay, EC50=0.028μM. | 18541726 | |||
| MT4 | Antiviral assay | Antiviral activity against Reverse transcriptase inhibitor-resistant Human immunodeficiency virus 1 infected in human MT4 cells assessed as inhibition of virus-induced cytopathic effect by MTT assay, EC50=0.029μM. | 18541726 | |||
| MT4 | Antiviral assay | Antiviral activity against non nucleoside reverse transcriptase inhibitor-resistant Human immunodeficiency virus 1 infected in human MT4 cells assessed as inhibition of virus-induced cytopathic effect by MTT assay, EC50=0.035μM. | 18541726 | |||
| MT4 | Antiretroviral assay | Antiretroviral activity against Human immunodeficiency virus 2 EHO infected in human MT4 cells assessed as inhibition of virus-induced cytopathic effect by MTT assay, EC50=0.049μM. | 18541726 | |||
| MT4 | Antiretroviral assay | Antiretroviral activity against Human immunodeficiency virus 2 ROD infected in human MT4 cells assessed as inhibition of virus-induced cytopathic effect by MTT assay, EC50=0.05μM. | 18541726 | |||
| MT4 | Antiretroviral assay | Antiretroviral activity against Simian immunodeficiency virus MAC 251 infected in human MT4 cells assessed as inhibition of virus-induced cytopathic effect by MTT assay, EC50=0.05μM. | 18541726 | |||
| MT4 | Antiviral assay | Antiviral activity against Protease inhibitor-resistant Human immunodeficiency virus 1 infected in human MT4 cells assessed as inhibition of virus-induced cytopathic effect by MTT assay, EC50=0.17μM. | 18541726 | |||
| MT4 | Antiviral assay | 5 uM | Antiviral activity against HIV1 NL4-3 harboring L10F/L33F/M46I/I47V/Q58E/V82I/I84V/I85V amino acid substitution in protease encoding region infected in human MT4 cells assessed as inhibition of p24 Gag protein production selected at 5 uM of GRL-02031 by E, EC50=0.011μM. | 18955518 | ||
| MT4 | Antiviral assay | Antiviral activity against HIV1 NL4-3 infected in human MT4 cells assessed as inhibition of p24 gag protein production by ELISA, EC50=0.018μM. | 18955518 | |||
| MT2 | Antiviral assay | 7 days | Antiviral activity against HIV1 LAI infected in human MT2 cells after 7 days by MTT assay, EC50=0.023μM. | 18955518 | ||
| MT4 | Antiviral assay | 5 uM | Antiviral activity against HIV1 NL4-3 harboring L10F/V32I/M46I/I54M//A71V/I84V amino acid substitution in protease encoding region infected in human MT4 cells assessed as inhibition of p24 Gag protein production selected at 5 uM of amprenavir by ELISA, EC50=0.17μM. | 18955518 | ||
| MT4 | Antiviral assay | 1 uM | Antiviral activity against HIV1 NL4-3 harboring L23I/K43I/M46I/I50L/G51A/A71V amino acid substitution in protease encoding region infected in human MT4 cells assessed as inhibition of p24 Gag protein production selected at 1 uM of atazanavir by ELISA, EC50=0.21μM. | 18955518 | ||
| MT4 | Antiviral assay | 5 uM | Antiviral activity against HIV1 NL4-3 harboring M46I/V82F/I84V amino acid substitution in protease encoding region infected in human MT4 cells assessed as inhibition of p24 Gag protein production selected at 5 uM of ritonavir by ELISA, EC50=0.24μM. | 18955518 | ||
| MT4 | Antiviral assay | 5 uM | Antiviral activity against HIV1 NL4-3 harboring L10I/G48V/I54V/L90M amino acid substitution in protease encoding region infected in human MT4 cells assessed as inhibition of p24 Gag protein production selected at 5 uM of saquinavir by ELISA, EC50=0.32μM. | 18955518 | ||
| MT4 | Antiviral assay | 1 uM | Antiviral activity against HIV1 NL4-3 harboring L10F/M46I/I54V/V82A amino acid substitution in protease encoding region infected in human MT4 cells assessed as inhibition of p24 Gag protein production selected at 1 uM of Lopinavir by ELISA, EC50=0.51μM. | 18955518 | ||
| MT4 | Antiviral assay | 5 uM | Antiviral activity against HIV1 NL4-3 harboring L10F/L24I/M46I/L63P/A71V/G73S/V82T amino acid substitution in protease encoding region infected in human MT4 cells assessed as inhibition of p24 Gag protein production selected at 5 uM of indinavir by ELISA, EC50=0.65μM. | 18955518 | ||
| HeLa | Antiviral assay | 72 hrs | Antiviral activity against HIV1 harboring capsid I201V mutant protein infected in human HeLa cells assessed as decrease in viral infection after 72 hrs by beta-galactosidase reporter gene assay, EC50=0.013μM. | 19805571 | ||
| HeLa | Antiviral assay | 72 hrs | Antiviral activity against wild type HIV1 infected in human HeLa cells assessed as decrease in viral infection after 72 hrs by beta-galactosidase reporter gene assay, EC50=0.016μM. | 19805571 | ||
| HeLa | Antiviral assay | 72 hrs | Antiviral activity against HIV1 harboring spacer peptide A1V mutant protein infected in human HeLa cells assessed as decrease in viral infection after 72 hrs by beta-galactosidase reporter gene assay, EC50=0.038μM. | 19805571 | ||
| cord blood mononuclear cells | Antiviral assay | 48 hrs | Antiviral activity against wild type HIV1 subtype C infected in human cord blood mononuclear cells assessed as inhibition of viral replication after 48 hrs by luciferase reporter gene assay, EC50=0.00167μM. | 20404123 | ||
| cord blood mononuclear cells | Antiviral assay | 48 hrs | Antiviral activity against wild type HIV1 subtype CRF02_AG infected in human cord blood mononuclear cells assessed as inhibition of viral replication after 48 hrs by luciferase reporter gene assay, EC50=0.0057μM. | 20404123 | ||
| cord blood mononuclear cells | Antiviral assay | 48 hrs | Antiviral activity against wild type HIV1 subtype B infected in human cord blood mononuclear cells assessed as inhibition of viral replication after 48 hrs by luciferase reporter gene assay, EC50=0.0098μM. | 20404123 | ||
| cord blood mononuclear cells | Antiviral assay | 48 hrs | Antiviral activity against HIV1 subtype CRF02_AG harboring protease polymorphism at I36 position and M46 mutant gene infected in human cord blood mononuclear cells assessed as inhibition of viral replication after 48 hrs by luciferase reporter gene assay, EC50=0.055μM. | 20404123 | ||
| cord blood mononuclear cells | Antiviral assay | 48 hrs | Antiviral activity against HIV1 subtype CRF02_AG harboring protease L33I, M46I, A71T mutant gene and polymorphism at M36 position infected in human cord blood mononuclear cells assessed as inhibition of viral replication after 48 hrs by luciferase reporte, EC50=0.202μM. | 20404123 | ||
| cord blood mononuclear cells | Antiviral assay | 48 hrs | Antiviral activity against HIV1 subtype C harboring protease L23I, M46I, L89T mutant gene and polymorphism at M36 position infected in human cord blood mononuclear cells assessed as inhibition of viral replication after 48 hrs by luciferase reporter gene , EC50=0.272μM. | 20404123 | ||
| cord blood mononuclear cells | Antiviral assay | 48 hrs | Antiviral activity against HIV1 subtype B harboring protease D30N, M46I, A71T and V77I mutant gene and polymorphism at M36 position of protease infected in human cord blood mononuclear cells assessed as inhibition of viral replication after 48 hrs by luci, EC50=1.139μM. | 20404123 | ||
| cord blood mononuclear cells | Antiviral assay | 48 hrs | Antiviral activity against HIV1 subtype B harboring protease D30N, L33I, M46I, N88D mutant gene and polymorphism at I36 position infected in human cord blood mononuclear cells assessed as inhibition of viral replication after 48 hrs by luciferase reporter, EC50=1.463μM. | 20404123 | ||
| cord blood mononuclear cells | Antiviral assay | 48 hrs | Antiviral activity against HIV1 subtype C harboring protease D30N, E35G, I85V, L90M mutant gene and polymorphism at I36 position infected in human cord blood mononuclear cells assessed as inhibition of viral replication after 48 hrs by luciferase reporter, EC50=3.473μM. | 20404123 | ||
| TZM-bl | Antiviral assay | 48 hrs | Antiviral activity against HIV1 subtype B harboring protease polymorphism at M36 position infected in human TZM-bl cells assessed as inhibition of viral replication after 48 hrs by luciferase reporter gene assay | 20404123 | ||
| TZM-bl | Antiviral assay | 48 hrs | Antiviral activity against HIV1 subtype CRF02_AG harboring protease polymorphism at I36 position infected in human TZM-bl cells assessed as inhibition of viral replication after 48 hrs by luciferase reporter gene assay | 20404123 | ||
| TZM-bl | Antiviral assay | 48 hrs | Antiviral activity against HIV1 subtype B harboring protease polymorphism at I36 position infected in human TZM-bl cells assessed as inhibition of viral replication after 48 hrs by luciferase reporter gene assay | 20404123 | ||
| MT4 | Antiviral assay | Antiviral activity against wild type HIV1 NL4-3 infected in human MT4 cells by MTT assay, EC50=0.045μM. | 20439612 | |||
| MT4 | Antiviral assay | Antiviral activity against HIV1 expressing protease L10I/L24I/M46I/V82I/I84V mutant infected in human MT4 cells selected after 50 passages of GRL-216 by MTT assay, EC50=0.13μM. | 20439612 | |||
| MT4 | Antiviral assay | 1 uM | Antiviral activity against HIV1 expressing protease L10F/M46M,I/Q61Q mutant infected in human MT4 cells selected at 1 uM of GRL-396 by MTT assay, EC50=0.22μM. | 20439612 | ||
| MT4 | Antiviral assay | 1 uM | Antiviral activity against HIV1 expressing protease L10F/M46I/T91S mutant infected in human MT4 cells selected at 1 uM of GRL-246 by MTT assay, EC50=0.29μM. | 20439612 | ||
| MT4 | Antiviral assay | 5 uM | Antiviral activity against HIV1 expressing protease L10F/M46I/I50V/A71V/I84V/L90M mutant infected in human MT4 cells selected at 5 uM of amprenavir by MTT assay, EC50=0.3μM. | 20439612 | ||
| MT4 | Antiviral assay | 5 uM | Antiviral activity against HIV1 expressing protease L10F/M46I/I54V/V82A mutant infected in human MT4 cells selected at 5 uM of Lopinavir by MTT assay, EC50=0.32μM. | 20439612 | ||
| MT4 | Antiviral assay | 1 uM | Antiviral activity against HIV1 expressing protease L10F/M46L/I50V/A71Vmutant infected in human MT4 cells selected at 1 uM of GRL-286 by MTT assay, EC50=0.37μM. | 20439612 | ||
| MT4 | Antiviral assay | 5 uM | Antiviral activity against HIV1 expressing protease L10I/G48V/I54V/A71V/I84V/L90M mutant infected in human MT4 cells selected at 5 uM of saquinavir by MTT assay, EC50=0.51μM. | 20439612 | ||
| BESM | Antitrypanosomal assay | 88 hrs | Antitrypanosomal activity against Trypanosoma cruzi amastigotes infected in BESM cells measured after 88 hrs postinfection by HTS assay, EC50=12μM. | 20547819 | ||
| BESM | Cytotoxicity assay | 88 hrs | Cytotoxicity against BESM cells after 88 hrs by HTS assay, EC50=32μM. | 20547819 | ||
| CMEC/D3 | Function assay | 30 mins | Inhibition of P-gp in human CMEC/D3 cells using NBD-Aba as substrate after 30 mins by flow cytometric analysis, IC50=1.7μM. | 31505928 | ||
| CMEC/D3 | Function assay | 30 mins | Inhibition of P-gp in human CMEC/D3 cells using calcein-AM as substrate after 30 mins by flow cytometric analysis, IC50=2μM. | 31505928 | ||
| 12D7-MDR | Function assay | 30 mins | Inhibition of P-gp in human 12D7-MDR cells using NBD-Aba as substrate after 30 mins by flow cytometric analysis, IC50=5.8μM. | 31505928 | ||
| 12D7-MDR | Function assay | 30 mins | Inhibition of P-gp in human 12D7-MDR cells using calcein-AM as substrate after 30 mins by flow cytometric analysis, IC50=9.1μM. | 31505928 | ||
| 12D7 | Antiviral assay | 3 days | Antiviral activity against HIV1 LAI infected in human 12D7 cells overexpressing p-gp assessed as reduction in P24 level at 1:1 ratio of test compound to abacavir incubated for 3 days followed by followed by replacement of fresh medium containing compound | 31505928 | ||
| 12D7 | Antiviral assay | 0.08 to 1.25 uM | 3 days | Antiviral activity against HIV1 LAI infected in human 12D7 cells overexpressing p-gp assessed as reduction in P24 level at 0.08 to 1.25 uM incubated for 3 days followed by replacement of fresh medium containing compound and measured after 3 days by ELISA | 31505928 | |
| SJ-GBM2 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SJ-GBM2 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 | |||
| U-2 OS | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for U-2 OS cells | 29435139 | |||
| Saos-2 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Saos-2 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 | |||
| MG 63 (6-TG R) | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for MG 63 (6-TG R) cells | 29435139 | |||
| MT2 | Antiviral assay | 5 days | Antiviral activity against wild type HIV1 3B infected in human MT2 cells assessed as virus-induced cytopathic effect after 5 days by XTT assay, EC50=0.0049μM. | ChEMBL | ||
| HepG2 | Cytotoxicity assay | 5 days | Cytotoxicity against human HepG2 cells assessed as reduction in cell viability after 5 days by XTT assay, CC50=7.4μM. | ChEMBL | ||
| skeletal myoblast cells | Cytotoxicity assay | 72 hours | DNDI: Cytotoxicity in Vitro, 72 hour, in rat skeletal myoblast cells, IC50=12.05μM. | ChEMBL | ||
| MT2 | Cytotoxicity assay | 5 days | Cytotoxicity against human MT2 cells assessed as reduction in cell viability after 5 days by XTT assay, CC50=19.1μM. | ChEMBL | ||
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Chemische Informationen, Lagerung & Stabilität
| Molekulargewicht | 663.89 | Formel | C33H49N3O7S2 |
Lagerung (Ab dem Eingangsdatum) | |
|---|---|---|---|---|---|
| CAS-Nr. | 159989-65-8 | SDF herunterladen | Lagerung von Stammlösungen |
|
|
| Synonyme | AG 1343 Mesylate | Smiles | CC1=C(C=CC=C1O)C(=O)NC(CSC2=CC=CC=C2)C(CN3CC4CCCCC4CC3C(=O)NC(C)(C)C)O.CS(=O)(=O)O | ||
Löslichkeit
|
In vitro |
DMSO
: 100 mg/mL
(150.62 mM)
Ethanol : 100 mg/mL Water : Insoluble |
Molaritätsrechner
Verdünnungsrechner
Molekulargewichtsrechner
|
In vivo |
|||||
In-vivo-Formulierungsrechner (Klare Lösung)
Schritt 1: Geben Sie die untenstehenden Informationen ein (Empfohlen: Ein zusätzliches Tier zur Berücksichtigung von Verlusten während des Experiments)
mg/kg
g
μL
Schritt 2: Geben Sie die In-vivo-Formulierung ein (Dies ist nur der Rechner, keine Formulierung. Bitte kontaktieren Sie uns zuerst, wenn es im Abschnitt "Löslichkeit" keine In-vivo-Formulierung gibt.)
% DMSO
%
% Tween 80
% ddH2O
%DMSO
%
Berechnungsergebnisse:
Arbeitskonzentration: mg/ml;
Methode zur Herstellung der DMSO-Stammlösung: mg Wirkstoff vorgelöst in μL DMSO ( Konzentration der Stammlösung mg/mL, Bitte kontaktieren Sie uns zuerst, wenn die Konzentration die DMSO-Löslichkeit der Wirkstoffcharge überschreitet. )
Methode zur Herstellung der In-vivo-Formulierung: Nehmen Sie μL DMSO Stammlösung, dann hinzufügenμL PEG300, mischen und klären, dann hinzufügenμL Tween 80, mischen und klären, dann hinzufügen μL ddH2O, mischen und klären.
Methode zur Herstellung der In-vivo-Formulierung: Nehmen Sie μL DMSO Stammlösung, dann hinzufügen μL Maisöl, mischen und klären.
Hinweis: 1. Bitte stellen Sie sicher, dass die Flüssigkeit klar ist, bevor Sie das nächste Lösungsmittel hinzufügen.
2. Achten Sie darauf, das/die Lösungsmittel der Reihe nach hinzuzufügen. Sie müssen sicherstellen, dass die bei der vorherigen Zugabe erhaltene Lösung eine klare Lösung ist, bevor Sie mit der Zugabe des nächsten Lösungsmittels fortfahren. Physikalische Methoden wie Vortex, Ultraschall oder ein heißes Wasserbad können zur Unterstützung des Lösens verwendet werden.
Wirkmechanismus
| Targets/IC50/Ki |
HIV protease
(Cell-free assay) 2 nM(Ki)
|
|---|---|
| In vivo |
In-vivo-Studien zeigen, dass AG1343 bei verschiedenen Spezies oral gut resorbiert wird und beim Menschen günstige pharmakokinetische Eigenschaften aufweist. Erste Untersuchungen der Verbindung an gefütterten Ratten ergaben eine orale Bioverfügbarkeit von 43 %. Im Gegensatz dazu war die orale Bioverfügbarkeit bei gefasteten Ratten signifikant auf 29 % reduziert. Nelfinavir zeigte eine signifikante orale Bioverfügbarkeit bei einer Reihe von Spezies, darunter Hunde (47 %), Marmosetten (17 %) und Cynomolgus-Affen (26 %). Es hat nach oraler Verabreichung eine lange Plasmahalbwertszeit, was wahrscheinlich auf eine Kombination aus langsamer Auflösung und Absorption zurückzuführen ist. Nelfinavir wird beim Menschen gut resorbiert, insbesondere wenn es mit Nahrung verabreicht wird, und weist minimale und leicht zu handhabende Nebenwirkungen auf.
|
Literatur |
Anwendungen
| Methoden | Biomarker | Bilder | PMID |
|---|---|---|---|
| Growth inhibition assay | Cell viability |
|
22271897 |
| Western blot | p-eIF2Aα / eIF2Aα / ATF4 / GRP78 / CHOP SOD1 / SOD2 / catalase PAX3 / MITF |
|
21697087 |
| Immunofluorescence | LC3 / p62 PAX3 / MITF p-SMAD2 |
|
27330277 |
Klinische Studieninformationen
(Daten von https://clinicaltrials.gov, aktualisiert am 2024-05-22)
| NCT-Nummer | Rekrutierung | Erkrankungen | Sponsor/Kooperationspartner | Startdatum | Phasen |
|---|---|---|---|---|---|
| NCT00051844 | Completed | Human Immunodeficiency Virus |
Pfizer |
August 2002 | Phase 2 |
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