1. Metabolic Enzyme/Protease
  2. Cytochrome P450

Cobicistat (Synonyms: GS-9350)

Cat. No.: HY-10493 Purity: >98.0%
Data Sheet SDS Handling Instructions

Cobicistat is a potent, and selective inhibitor of cytochrome P450 3A (CYP3A) enzymes with IC50 of 30-285 nM.

For research use only. We do not sell to patients.
Cobicistat Chemical Structure

Cobicistat Chemical Structure

CAS No. : 1004316-88-4

Size Price Stock Quantity
Free Sample (0.5-1 mg)   Apply now  
10 mM * 1 mL in DMSO $184 In-stock
5 mg $175 In-stock
10 mg $215 In-stock
50 mg $750 In-stock
100 mg $1250 In-stock
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  • Biological Activity

  • Protocol

  • Technical Information

  • Purity & Documentation

  • References

Description

Cobicistat is a potent, and selective inhibitor of cytochrome P450 3A (CYP3A) enzymes with IC50 of 30-285 nM.

IC50 & Target

IC50: 30-285 nM (Cytochrome P450)[1]

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 > 30 μM 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]. Cobicistat is a novel cytochrome P450 3A4 inhibitor in advanced clinical evaluation for use as a pharmacoenhancer of antiretroviral drugs. It lacks significant anti-HIV activity and is more selective than ritonavir in its enzyme inhibition[2].

Clinical Trial
NCT Number Sponsor Condition Start Date Phase
NCT02503462 University Hospital, Basel, Switzerland AIDS-related Dementia Complex July 2015 Phase 4
NCT03123848 Janssen Pharmaceutical K.K. Healthy April 14, 2017 Phase 4
NCT02818348 Fundacio Lluita Contra la SIDA HIV-1 Infection June 2016 Phase 1
NCT01619527 Janssen R&D Ireland Healthy Participants April 2012 Phase 1
NCT02404233 Therapeutic Concepts|Janssen Scientific Affairs, LLC HIV Positive March 2015 Phase 4
NCT01837719 Bristol-Myers Squibb Human Immunodeficiency Virus Type 1 (HIV-1) April 2013 Phase 1
NCT02578550 Janssen Sciences Ireland UC Healthy November 2015 Phase 1
NCT02307656 Bristol-Myers Squibb HIV in Adults November 21, 2014 Phase 1
NCT02499978 Stanford University|Janssen Scientific Affairs, LLC|University of Colorado, Denver HIV/AIDS May 2016 Phase 2|Phase 3
NCT00855335 Janssen Scientific Affairs, LLC HIV|HIV Infections|Pregnancy April 2009 Phase 3
NCT02565888 Radboud University Hepatitis C|HIV November 2015 Phase 1
NCT01896622 National Institutes of Health Clinical Center (CC)|National Institute of Allergy and Infectious Diseases (NIAID) HIV June 18, 2013 Phase 1
NCT02219217 St Stephens Aids Trust|ViiV Healthcare HIV October 2014 Phase 1
NCT02016924 Gilead Sciences Acquired Immune Deficiency Syndrome (AIDS)|HIV Infections January 16, 2014 Phase 2|Phase 3
NCT02475135 Janssen Sciences Ireland UC Healthy June 2015 Phase 1
NCT02431247 Janssen Sciences Ireland UC Immunodeficiency Virus Type 1, Human July 6, 2015 Phase 3
NCT03045861 GlaxoSmithKline Infection, Human Immunodeficiency Virus March 17, 2017 Phase 2
NCT02198443 Fundacion Clinic per a la Recerca Biomédica HIV June 6, 2015 Phase 4
NCT02984852 Janssen Scientific Affairs, LLC Healthy December 2016 Phase 1
NCT02771249 National Institutes of Health Clinical Center (CC) Healthy Volunteers May 5, 2016 Phase 1
NCT02987530 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 HIV-1 Infection January 2017 Phase 3
NCT02277600 ViiV Healthcare|GlaxoSmithKline Drug-drug Interaction Study November 5, 2014 Phase 1
NCT02180438 University of Washington|Clinique des Maladies Infectieuses Ibrahima DIOP Mar/CRCF, Centre Hospitalier Universitaire de Fann|Gilead Sciences HIV-2 Infection September 2014 Phase 4
NCT02351908 St Stephens Aids Trust|Merck Sharp & Dohme Corp. HIV March 2015 Phase 4
NCT01929759 Massachusetts General Hospital|Brigham and Women's Hospital|Gilead Sciences HIV Disease January 2014
NCT03163277 Giovanni Di Perri|University of Turin, Italy Hiv|Neurocognitive Dysfunction May 15, 2017 Phase 4
NCT02859558 AIDS Clinical Trials Group|National Institute of Allergy and Infectious Diseases (NIAID) HIV-1 Infection January 2017 Phase 2
NCT02625207 ViiV Healthcare|Pfizer Healthy Subjects November 6, 2015 Phase 1
NCT02397096 Merck Sharp & Dohme Corp. HIV-1 Infection June 9, 2015 Phase 3
NCT02470650 Juan A. Arnaiz|Hospital Clinic of Barcelona Patient Compliance|Antiretroviral Therapy Intolerance June 2015 Phase 4
NCT02203461 Technische Universität München|Gilead Sciences|MUC Research GmbH Insulin Resistance July 2014 Phase 1
NCT00042289 National Institute of Allergy and Infectious Diseases (NIAID)|Eunice Kennedy Shriver National Institute of Child Health and Human Development (NICHD) HIV Infections March 2003 Phase 4
NCT00537966 University of Zurich HIV Infections January 2002
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References
Preparing Stock Solutions
Concentration Volume (DMSO) Mass 1 mg 5 mg 10 mg
1 mM 1.2886 mL 6.4431 mL 12.8863 mL
5 mM 0.2577 mL 1.2886 mL 2.5773 mL
10 mM 0.1289 mL 0.6443 mL 1.2886 mL
Kinase Assay
[1]

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°C and the reaction initiated by the addition of an NADPH generating system followed by further incubation at 37°C 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. MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Assay
[1]

Five-fold serial dilutions of the tested compounds are prepared in triplicate in 96-well plates. MT-2 cells are added to plates at a density of 20,000/well in a final assay volume of 200 μL. After a 5-day incubation at 37°C, the cytotoxic effect is determined using a cell viability assay. One hundred μL media is removed from each well and replaced with 100 μL of phosphate-buffered saline containing 1.7 mg/mL XTT and 5 μg/mL PMS. Following 1-hour incubation at 37°C, 20 μL of 2% Triton X- 100 is added to each well and absorbance is read at 450 nm with a background subtraction at 650 nm. The data are plotted as cell viability vs. drug concentration. Cell viability is expressed as a percentage of the signal from untreated samples (0% cytotoxicity) after the subtraction of signal from samples treated with 10 μM of Podophyllotoxin (100% cytotoxicity). The CC50 value is calculated from the inhibition plots as the concentration of drug which inhibits cell proliferation by 50%. MCE has not independently confirmed the accuracy of these methods. They are for reference only.

References
Molecular Weight

776.02

Formula

C₄₀H₅₃N₇O₅S₂

CAS No.

1004316-88-4

Storage
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
Shipping

Room temperature in continental US; may vary elsewhere

Solvent & Solubility

DMSO: ≥ 29 mg/mL

* "<1 mg/mL" means slightly soluble or insoluble. "≥" means soluble, but saturation unknown.

Purity: >98.0%

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Cobicistat
Cat. No.:
HY-10493
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