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Purity: ≥98%
Cobicistat (trade name Tybost; Genvoya; GS-9350; GS 9350) is a novel, potent and selective inhibitor of CYP3A (cytochrome P450 3A) with IC50 of 30-285 nM. It is used in combination with other anti-HIV drugs to boost/increase the levels of certain HIV protease inhibitors (atazanavir and darunavir) which are metabolized by CYP3A enzymes, by inhibiting these enzymes.
| ln Vitro |
In both antiviral cellular tests and HIV-1 protease enzymatic assays, cobicistat is inactive against HIV-1 protease (IC50>30 μM). Cobicistat did not reduce HIV replication in a multi-cycle, five-day MT-2 HIV infection experiment (EC50>30 μM). Cobicistat demonstrated no cytotoxicity in tests on MT-2 cells, with CC50 values greater than 80 μM [1]. Ritonavir and Cobicistat inhibit CYP3A via the same mechanism. It implies that the heme group of the CYP3A enzyme may be directly involved in its inhibitory action on CYP3A [1]. In experiments measuring lipid accumulation in human adipocytes, ritonavir demonstrated noteworthy effects, with an EC50 of 16 μM. At doses as high as 30 μM, however, Cobicistat had no effect [1]. When tested at a concentration of 10 μM, ritonavir significantly affected mouse adipocyte glucose absorption assays. Conversely, Cobicistat (10 μM) has a much smaller impact on the absorption of glucose [1].
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| References |
[1]. 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
[2]. Temesgen Z. Cobicistat, a pharmacoenhancer for HIV treatments. Drugs Today (Barc). 2013 Apr;49(4):233-7 |
| Molecular Formula |
C40H53N7O5S2
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| Molecular Weight |
776.02
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| CAS # |
1004316-88-4
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| Related CAS # |
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| SMILES |
O=C(OCC1=CN=CS1)N[C@H](CC[C@@H](NC([C@@H](NC(N(CC2=CSC(C(C)C)=N2)C)=O)CCN3CCOCC3)=O)CC4=CC=CC=C4)CC5=CC=CC=C5
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| InChi Key |
ZCIGNRJZKPOIKD-CQXVEOKZSA-N
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| InChi Code |
InChI=1S/C40H53N7O5S2/c1-29(2)38-43-34(27-53-38)25-46(3)39(49)45-36(16-17-47-18-20-51-21-19-47)37(48)42-32(22-30-10-6-4-7-11-30)14-15-33(23-31-12-8-5-9-13-31)44-40(50)52-26-35-24-41-28-54-35/h4-13,24,27-29,32-33,36H,14-23,25-26H2,1-3H3,(H,42,48)(H,44,50)(H,45,49)/t32-,33-,36+/m1/s1
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| Chemical Name |
thiazol-5-ylmethyl ((2R,5R)-5-((S)-2-(3-((2-isopropylthiazol-4-yl)methyl)-3-methylureido)-4-morpholinobutanamido)-1,6-diphenylhexan-2-yl)carbamate
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| Synonyms |
Cobicistat; GS9350; trade name: Tybost; Genvoya; GS-9350; GS 9350;
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
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| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
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| Preparing Stock Solutions | 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 |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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