Name: Cobicistat (GS-9350)
Price: 306.00 USD

- Overview
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    Background
    
    Cobicistat is a selective inhibitor of cytochrome P450 (CYP) 3A enzymes with IC50 values ranging from 0.03 to 0.285μM [1].Cobicistat is a selective CYP3A inhibitor without intrinsic anti-HIV activity and is indicated in EU as a pharmacokinetic enhancer of the HIV-1 protease inhibitors atazanavir and darunavir in adults. Cobicistat is also developed to form a fixed-dose tablet in combination with elvitegravir, emtricitabine and TDF. Cobicistat inhibits CYP3A in vitro across a variety of substrates with IC50 values ranging from 0.03 to 0.285μM. Cobicistat is absorbed rapidly after oral administration in patients infected with HIV-1 with the Cmax of 1.2μg/ml. In the 48-week analysis of the phase III study, once-daily oral cobicistat is generally well tolerated. The tolerability of the cobicistat-boosted atazanavir remains similar longer term, with jaundice, ocular icterus and nausea in a 96-week analysis of the phase III study [1].
    
    [1] Deeks ED. Cobicistat: a review of its use as a pharmacokinetic enhancer of atazanavir and darunavir in patients with HIV-1 infection. Drugs. 2014 Feb;74(2):195-206.
- Properties
  - Alternative Name
    
    thiazol-5-ylmethyl (5-(2-(3-((2-isopropylthiazol-4-yl)methyl)-3-methylureido)-4-morpholinobutanamido)-1,6-diphenylhexan-2-yl)carbamate
    
    CAS Number
    
    1004316-88-4
    
    Molecular Formula
    
    C40H53N7O5S2
    
    Molecular Weight
    
    776.02
    
    Appearance
    
    A solid
    
    Purity
    
    98.00%
    
    Solubility
    
    insoluble in H2O; ≥150.9 mg/mL in DMSO; ≥102.4 mg/mL in EtOH with ultrasonic
    
    Storage
    
    Store at -20°C
    
    * For Research Use Only