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

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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
200 mg   Get quote  
500 mg   Get quote  

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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].

References
Preparing Stock Solutions
Concentration Volume 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
Please refer to the solubility information to select the appropriate solvent.
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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Product Name:
Cobicistat
Cat. No.:
HY-10493
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