| Cobicistat (GS-9350)Selective CYP3A inhibitor |
Sample solution is provided at 25 µL, 10mM.
Nature.2017 Jan 19;541(7637):417-420.
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- Purity = 99.76%
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Chemical structure
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| Cas No. | 1004316-88-4 | SDF | Download SDF |
| Chemical Name | thiazol-5-ylmethyl (5-(2-(3-((2-isopropylthiazol-4-yl)methyl)-3-methylureido)-4-morpholinobutanamido)-1,6-diphenylhexan-2-yl)carbamate | ||
| Canonical SMILES | CC(C1=NC(CN(C(NC(C(NC(CC2=CC=CC=C2)CCC(NC(OCC3=CN=CS3)=O)CC4=CC=CC=C4)=O)CCN5CCOCC5)=O)C)=CS1)C | ||
| Formula | C40H53N7O5S2 | M.Wt | 776.02 |
| Solubility | ≥150.9 mg/mL in DMSO, ≥102.4 mg/mL in EtOH with ultrasonic, <2.22 mg/ml="" in="" h2o=""> | Storage | Store at -20°C |
| Physical Appearance | A solid | Shipping Condition | Evaluation sample solution : ship with blue ice.All other available size:ship with RT , or blue ice upon request |
| General tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months. | ||
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].
References:[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.
