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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Effects of rifampin alone or in combination with cobicistat on the mean DRV CLint.app. in primary human hepatocytes in vitro. Cryopreserved primary human hepatocytes were incubated with RIF (0.5 to 20 μM) (hatched bars) or with COBI (0.13 to 12.76 μM) and RIF (0.5 to 20 μM) (gray bars) for 72 h. All cells were then incubated with RIF (0.5 to 20 M) or RIF (0.5 to 20 μM) together with COBI (0.13 to 12.76 μM), as described above, together with DRV (5 μM) for 60 min. Control cells were treated with DRV (5 μM) alone for 60 min (black bar). The results shown represent the mean DRV CLint.app. from three biological replicates measured in hepatocytes from three independent donors (donors HU1399, HU1574, and HU1587). Error bars indicate SDs.
Antimicrob Agents Chem, 2017, doi:10.1128/AAC.01776-16. Cobicistat (GS-9350) purchased from Selleck.
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|Description||Cobicistat (GS-9350) is a potent and selective inhibitor of CYP3A with IC50 of 30-285 nM.|
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. 
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.
|In vitro||DMSO||100 mg/mL (128.86 mM)|
|Ethanol||100 mg/mL (128.86 mM)|
|In vivo||Add solvents to the product individually and in order(Data is from Selleck tests instead of citations):
5% DMSO+40% PEG 300+ddH2O
For best results, use promptly after mixing.
* 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.
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Clinical Trial Information
|NCT Number||Recruitment||interventions||Conditions||Sponsor/Collaborators||Start Date||Phases|
|NCT03094507||Completed||Drug: Tivicay|Drug: Rezolsta||HIV||St Stephens Aids Trust|ViiV Healthcare||April 19 2017||Phase 1|
|NCT03101644||Completed||Drug: Darunavir||Human Immunodeficiency Virus I Infection||Université Catholique de Louvain|Cliniques universitaires Saint-Luc- Université Catholique de Louvain||March 23 2017||Phase 4|
|NCT03042390||Completed||--||HIV Infections||Fundacion SEIMC-GESIDA|Janssen-Cilag S.A.||December 23 2016||--|
|NCT02697851||Terminated||Drug: Microgynon 30®|Drug: Evotaz®||HIV||St Stephens Aids Trust|Bristol-Myers Squibb||July 2016||Phase 1|
|NCT02818348||Completed||Drug: darunavir/cobicistat|Drug: etravirine||HIV-1 Infection||Fundacio Lluita Contra la SIDA||June 2016||Phase 1|
|NCT02600819||Active not recruiting||Drug: E/C/F/TAF|Drug: B/F/TAF||HIV-1 Infection||Gilead Sciences||December 14 2015||Phase 3|
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.
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