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Cobicistat P450 (e.g. CYP17) inhibitor

Cat.No.S2900

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

Batch: Purity: 99.25%
99.25

Solubility

In vitro
Batch:

DMSO : 100 mg/mL (128.86 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Ethanol : 100 mg/mL

Water : Insoluble

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In vivo
Batch:

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Working concentration: mg/ml;

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.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Chemical Information, Storage & Stability

Molecular Weight 776.02 Formula

C40H53N7O5S2

Storage (From the date of receipt)
CAS No. 1004316-88-4 Download SDF Storage of Stock Solutions

Synonyms GS-9350 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

Read more about storage stability stock solution CAS number SMILES

Mechanism of Action

Targets/IC50/Ki
CYP3A
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.
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.
References

Clinical Trial Information

(data from https://clinicaltrials.gov, updated on 2026-06-10)

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT06337032 RECRUITING
HIV-1-infection
Gilead Sciences
2024-08-27 PHASE4
NCT06014489 RECRUITING
AML, Adult
Stichting Hemato-Oncologie voor Volwassenen Nederland
2024-01-17 PHASE2
NCT04065399 RECRUITING
Acute Myeloid Leukemia; Acute Lymphoblastic Leukemia; Mixed Lineage Acute Leukemia; Mixed Phenotype Acute Leukemia; Acute Leukemia of Ambiguous Lineage
Syndax Pharmaceuticals
2019-11-05 PHASE1; PHASE2
NCT07462559 NOT_YET_RECRUITING
Drug Drug Interaction
Helsinki University Central Hospital
2026-03-04 PHASE1
NCT07678268 RECRUITING
HIV Infection; Antiretroviral Therapy; Lentivirus Infections
Instituto Mexicano del Seguro Social
2025-07-10 PHASE4
NCT05748093 UNKNOWN
Non-small Cell Lung Cancer
Maastricht University Medical Center
2024-04-01 PHASE4

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