Home Metabolism P450 (e.g. CYP17) inhibitor Cobicistat For research use only.

Cobicistat

Synonyms: GS-9350

Cobicistat is a potent and selective inhibitor of CYP3A with IC50 of 30-285 nM.

Cobicistat Chemical Structure

Cobicistat Chemical Structure

CAS No. 1004316-88-4

Purity & Quality Control

Cobicistat Related Products

Signaling Pathway

P450 (e.g. CYP17) Signaling Pathways

P450 (e.g. CYP17) Signaling Pathway

Biological Activity

Description Cobicistat is a potent and selective inhibitor of CYP3A with IC50 of 30-285 nM.
Targets
CYP3A [1]
30 nM-285 nM
In vitro
In vitro Cobicistat (GS-9350) is a potent, and selective inhibitor of human cytochrome P450 3A (CYP3A) enzymes as a pharmacoenhancer. GS-9350 inhibits CYP3A with IC50 spectrum from 30 nM to 285 nM. In contrast to ritonavir, GS-9350 is devoid of anti-HIV activity, with IC50 of > 30μM against HIV-1 protease and EC50 of > 30μM in MT-2 HIV infection assay, and is thus more suitable for use in boosting anti-HIV drugs without risking selection of potential drug-resistant HIV variants. GS-9350 shows reduced liability for drug interactions and may have potential improvements in tolerability over ritonavir. [1]
Kinase Assay Cytochrome P450 Inhibition
Inhibition of human cytochrome P450 activities is determined in duplicate in pooled human hepatic microsomal fractions following current scientific and regulatory guidelines. Reaction conditions are linear with respect to incubation time and hepatic microsomal protein concentration. Substrates are present at concentrations equal to or less than their respective Km values determined under the same reaction conditions. Metabolite and/or substrate concentrations are determined using specific, internal standard controlled HPLC MS/MS assays. For reactions monitoring metabolite formation there is less than 20% consumption of substrate during the reaction. Unless otherwise noted microsomal fraction, diluted in potassium phosphate buffer, is preincubated with substrate and inhibitor for 5 min at 37 ℃ and the reaction initiated by the addition of an NADPH generating system followed by further incubation at 37 ℃ with shaking. Enzyme-selective positive control inhibitors are tested in parallel. At appropriate times aliquots of the mixture are removed and the reaction terminated by addition to a mixture of methanol and acetonitrile containing the respective internal standard. After centrifugation aliquots of the supernatant are subjected to HPLC-MS/MS analysis.
NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT06014489 Recruiting
AML Adult
Stichting Hemato-Oncologie voor Volwassenen Nederland
 January 17 2024 Phase 2
NCT05197075 Completed
Human Immunodeficiency Virus (HIV)
Janssen Research & Development LLC
 August 3 2022 Phase 1
NCT05378906 Completed
Healthy
Janssen Research & Development LLC
 June 7 2022 Phase 1

Chemical Information & Solubility

Molecular Weight 776.02 Formula

C40H53N7O5S2
CAS No. 1004316-88-4 SDF Download Cobicistat SDF
Smiles CC(C)C1=NC(=CS1)CN(C)C(=O)NC(CCN2CCOCC2)C(=O)NC(CCC(CC3=CC=CC=C3)NC(=O)OCC4=CN=CS4)CC5=CC=CC=C5
Storage (From the date of receipt)

In vitro
Batch:

DMSO : 100 mg/mL ( (128.86 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Ethanol : 100 mg/mL

Water : Insoluble


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In vivo
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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

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Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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