Cobicistat | CAS:1004316-88-4

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Name:Cobicistat; GS-9350
Cat. No. :CS-0742
CAS No. :1004316-88-4
Formula:C40H53N7O5S2
M. Wt. : 776.02
Solubility:DMSO: ≥ 29 mg/mL

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].

Temesgen Z. Cobicistat, a pharmacoenhancer for HIV treatments. Drugs Today (Barc). 2013 Apr;49(4):233-7. Lianhong Xu, et al. Cobicistat (GS-9350): A Potent and Selective Inhibitor of Human CYP3A as a Novel Pharmacoenhancer. ACS Med. Chem. Lett., 2010, 1 (5), pp 209–213