uitsluitend voor onderzoeksdoeleinden
Cat.Nr.S2271
| Gerelateerde doelwitten | Integrase Bacterial Antibiotics Fungal Antiviral COVID-19 Parasite Reverse Transcriptase HIV HCV Protease |
|---|---|
| Overige Anti-infection Inhibitoren | Clorsulon Sodium Tauroursodeoxycholate (TUDC) Ascomycin (FK520) p-Coumaric Acid Cystamine dihydrochloride LL37 (Human cathelicidin) Cetylpyridinium Chloride Chlorquinaldol Cetrimonium Bromide (CTAB) Cinchonidine |
| Cellijnen | Assaytype | Concentratie | Incubatietijd | Formulering | Activiteitsbeschrijving | PMID |
|---|---|---|---|---|---|---|
| MRC5 cells | Function assay | Antiviral activity against HCMV in MRC5 cells by plaque reduction assay, IC50=0.68 μM | ||||
| MRC5 cells | Proliferation assay | 10 μM | 54 hrs | Inhibition of HCMV proliferation in MRC5 cells after 54 hrs post-infection at 10 uM by plaque assay | ||
| MRC5 cells | Proliferation assay | 10 μM | 24 h | Inhibition of HCMV proliferation in MRC5 cells after 24 hrs post-infection at 10 uM by plaque assay | ||
| Bel7402 cells | Function assay | 12 h | Induction of LDLR protein in human Bel7402 cells after 12 hrs by RT-PCR assay relative to control | |||
| HepG2 cells | Function assay | 10 ug/mL | 12 h | Induction of LDLR protein expression in human HepG2 cells at 10 ug/mL after 12 hrs by flow cytometry | ||
| KB cells | Cytotoxicity assay | 72 h | Cytotoxicity against human KB cells after 72 hrs, IC50=7.32 μM | |||
| HL60 cells | Apoptosis assay | 48 hrs | Induction of apoptosis in human HL60 cells after 48 hrs using annexin V-propidium iodide staining by FACS analysis | |||
| A549 cells | Cytotoxicity assay | Cytotoxicity against human A549 cells by SRB assay, IC50=6.27 μM | ||||
| SKOV3 cells | Cytotoxicity assay | Cytotoxicity against human SKOV3 cells by SRB assay, IC50=16.44 μM | ||||
| SK-MEL-2 cells | Cytotoxicity assay | Cytotoxicity against human SK-MEL-2 cells by SRB assay, IC50=13.76 μM | ||||
| HCT15 cells | Cytotoxicity assay | Cytotoxicity against human HCT15 cells by SRB assay, IC50=16.59 μM | ||||
| CEM cells | Cytotoxicity assay | 48 hrs | Cytotoxicity against human CEM cells expressing green fluorescent protein after 48 hrs by MTT assay, CC50=2.09 μM | |||
| human CEM cells | Function assay | 7 days | Antiviral activity against 0.05 MOI Human immunodeficiency virus 1 NL4.3 infected in human CEM cells expressing green fluorescent protein assessed as p24 antigen production measured 7 days post infection by ELISA, EC50=0.13 μM | |||
| SKN cells | Growth inhibition assay | 72 h | Growth inhibition against human SKN cells after 72 hrs by MTT assay, GI50=15.88 μM | |||
| RKN cells | Growth inhibition assay | 48 hrs | Growth inhibition against human RKN cells after 48 hrs by MTT assay, GI50=49.6 μM | |||
| G402 cells | Growth inhibition assay | 48 hrs | Growth inhibition against human G402 cells after 48 hrs by MTT assay, GI50=11.87 μM | |||
| A10 cells | Function assay | 30 μM | 24 hrs | Downregulation of Scd2 mRNA expression in rat A10 cells at 30 uM after 24 hrs by quantitative RT-PCR analysis | ||
| A10 cells | Function assay | 30 μM | 24 hrs | Down regulation of Prim2 mRNA expression in rat A10 cells at 30 uM after 24 hrs by quantitative RT-PCR analysis | ||
| A10 cells | Function assay | 30 μM | 24 hrs | Downregulation of Impk mRNA expression in rat A10 cells at 30 uM after 24 hrs by quantitative RT-PCR analysis | ||
| HepG2-A16-CD81 cells | Function assay | 10 μM | NOVARTIS: Antimalarial liver stage activity measured as a greater than 50% reduction in Plasmodium yoelii schizont area in HepG2-A16-CD81 cells at 10uM compound concentration, determined by immuno-fluorescence. | |||
| HepG2-A16-CD81 cells | Function assay | 10 μM | NOVARTIS: Antimalarial liver stage activity measured as reduction in Plasmodium yoelii schizont area in HepG2-A16-CD81 cells by immuno-fluorescence, and median schizont size at 10uM compound concentration, IC50=0.548 μM | |||
| HepG2 cells | Function assay | 10 μM | 4 h | Increase in AMPKalpha phosphorylation in human HepG2 cells at 10 uM after 4 hrs by Western blot analysis relative to untreated control | ||
| HepG2 cells | Function assay | 10 μM | 4 h | Increase in total AMPKalpha level in human HepG2 cells at 10 uM after 4 hrs by Western blot analysis relative to untreated control | ||
| HepG2 cells | Function assay | 20 μM | 24 hrs | Induction of apoptosis in human HepG2 cells assessed as morphological changes at 20 uM after 24 hrs using Hoechst 33258 staining by fluorescence microscopic analysis | ||
| HT-29 cells | Cytotoxicity assay | 48 hrs | Cytotoxicity against human HT-29 cells after 48 hrs by MTT assay, IC50=8.45 μM | |||
| HepG2 cells | Cytotoxicity assay | 24 hrs | Cytotoxicity against human HepG2 cells after 24 hrs by MTT assay, IC50=11.22 μM | |||
| HepG2 cells | Cytotoxicity assay | 48 hrs | Cytotoxicity against human HepG2 cells after 48 hrs by MTT assay, IC50=8.32 μM | |||
| Klik om meer experimentele gegevens over de cellijn te bekijken | ||||||
| Moleculair gewicht | 371.81 | Formule | C20H18NO4.Cl |
Opslag (Vanaf de ontvangstdatum) | |
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| CAS-nr. | 633-65-8 | SDF downloaden | Opslag van stamoplossingen |
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In vitro |
DMSO
: 25 mg/mL
(67.23 mM)
Water : Insoluble Ethanol : Insoluble |
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In vivo |
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Stap 1: Voer de onderstaande informatie in (Aanbevolen: Een extra dier voor het geval van verlies tijdens het experiment)
Stap 2: Voer de in vivo formulering in (Dit is alleen de calculator, geen formulering. Neem eerst contact met ons op als er geen in vivo formulering is in het gedeelte Oplosbaarheid.)
Berekeningsresultaten:
Werkconcentratie: mg/ml;
Methode voor het bereiden van DMSO-mastervloeistof: mg geneesmiddel vooraf opgelost in μL DMSO ( Concentratie mastervloeistof mg/mL, Neem eerst contact met ons op als de concentratie de DMSO-oplosbaarheid van de partij geneesmiddel overschrijdt. )
Methode voor het bereiden van in vivo formulering: Neem μL DMSO mastervloeistof, voeg vervolgens toeμL PEG300, mengen en helder maken, voeg vervolgens toeμL Tween 80, mengen en helder maken, voeg vervolgens toe μL ddH2O, mengen en helder maken.
Methode voor het bereiden van in vivo formulering: Neem μL DMSO mastervloeistof, voeg vervolgens toe μL Maïsolie, mengen en helder maken.
Opmerking: 1. Zorg ervoor dat de vloeistof helder is voordat u het volgende oplosmiddel toevoegt.
2. Zorg ervoor dat u het/de oplosmiddel(en) in de juiste volgorde toevoegt. U moet ervoor zorgen dat de verkregen oplossing, bij de vorige toevoeging, een heldere oplossing is voordat u verdergaat met het toevoegen van het volgende oplosmiddel. Fysische methoden zoals vortexen, echografie of een warmwaterbad kunnen worden gebruikt om het oplossen te bevorderen.
| Targets/IC50/Ki |
Caspase-3
Caspase-8
PARP
cytochrome c
cIAP1
Bcl-2
Bcl-xL
JNK
p38 MAPK
ROS
Topo I
Topo II
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| In vitro |
Vergeleken met regorafenib alleen, remt de gecombineerde behandeling van Berberine (BBR) en regorafenib de proliferatie van hepatocellulaire carcinoom (HCC) cellen significant en induceert het cellulaire apoptosis. |
| In vivo |
De gecombineerde behandelingsgroep met Berberine (BBR) en regorafenib heeft een drastisch remmend effect op de groei van hepatocellulaire carcinoom (HCC) xenograft tumoren in naakte muizen. De verhoogde apoptosis van xenograft tumoren wordt waargenomen in de gecombineerde behandelingsgroep. |
Referenties |
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(gegevens van https://clinicaltrials.gov, bijgewerkt op 2024-05-22)
| NCT-nummer | Rekrutering | Aandoeningen | Sponsor/Medewerkers | Startdatum | Fasen |
|---|---|---|---|---|---|
| NCT06273241 | Not yet recruiting | Pharmacokinetic Study in Healthy Volunteers |
University Medicine Greifswald |
March 4 2024 | Not Applicable |
| NCT05845931 | Recruiting | Pharmacokinetic Study in Healthy Volunteers |
University Medicine Greifswald |
May 5 2023 | Not Applicable |
| NCT05480670 | Completed | Polycystic Ovary Syndrome |
Ayub Teaching Hospital |
November 1 2022 | Not Applicable |
| NCT05463003 | Completed | Pharmacokinetic Study in Healthy Volunteers |
University Medicine Greifswald |
July 19 2022 | Not Applicable |
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