Cobicistat (GS-9350)

Catalog No.S2900

Cobicistat (GS-9350) Chemical Structure

Molecular Weight(MW): 776.02

Cobicistat (GS-9350) is a potent and selective inhibitor of CYP3A with IC50 of 30-285 nM.

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Biological Activity

Description Cobicistat (GS-9350) is a potent and selective inhibitor of CYP3A with IC50 of 30-285 nM.
Targets
CYP3A [1]
30 nM-285 nM
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]

Protocol

Kinase Assay:[1]
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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.

Solubility (25°C)

In vitro DMSO 100 mg/mL (128.86 mM)
Ethanol 100 mg/mL (128.86 mM)
Water Insoluble
In vivo Add solvents to the product individually and in order:
5% DMSO+40% PEG 300+ddH2O
10mg/mL

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 776.02
Formula

C40H53N7O5S2

CAS No. 1004316-88-4
Storage powder
Synonyms N/A

Bio Calculators

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Clinical Trial Information

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT02771249 Suspended Healthy Volunteers National Institutes of Health Clinical Center (CC) May 5, 2016 Phase 1
NCT03045861 Not yet recruiting Infection, Human Immunodeficiency Virus GlaxoSmithKline February 2017 Phase 2
NCT02987530 Not yet recruiting HIV-1 Infection French National Institute for Health and Medical Research-French National Agency for Research on AIDS and Viral Hepatitis (Inserm-ANRS)|Institut National de la Santé Et de la Recherche Médicale, France January 2017 Phase 3
NCT02984852 Recruiting Healthy Janssen Scientific Affairs, LLC December 2016 Phase 1
NCT02859558 Not yet recruiting HIV-1 Infection AIDS Clinical Trials Group|National Institute of Allergy and Infectious Diseases (NIAID) August 2016 Phase 2
NCT02818348 Completed HIV-1 Infection Fundacio Lluita Contra la SIDA June 2016 Phase 1

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

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

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P450 (e.g. CYP17) Signaling Pathway Map

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID