Cobicistat

SKU: orb1300941

Description

Cobicistat

Research Area

Infectious Disease & Virology, Metabolism Research, Protein Biochemistry

Key Properties

• CAS Number: 1004316-88-4
• MW: 776.02
• Purity: 99.62%
• Formula: C₄₀H₅₃N₇O₅S₂
• SMILES: CC(C)c1nc(CN(C)C(=O)N[C@@H](CCN2CCOCC2)C(=O)N[C@H](CC[C@H](Cc2ccccc2)NC(=O)OCc2cncs2)Cc2ccccc2)cs1
• Target: Cytochromes P450,HIV Protease
• Solubility: Ethanol:93 mg/mL (119.84 mM);10% DMSO+40% PEG300+5% Tween 80+45% Saline:3.3 mg/mL (4.25 mM);H2O:< 1 mg/mL (insoluble or slightly soluble);DMSO:93 mg/mL (119.84 mM)

Bioactivity

• Target IC50:
  CYP3A:30 nM-285 nM
• 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 > 30 μM 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.
• Cell Research:
  Five-fold serial dilutions o the tested compounds are prepared in triplicate in 96-well plates. MT-2 cells are added to plates at a density of 20,000/well in a final assay volume of 200 μL. After a 5-day incubation at 37℃he cytotoxic effect is determined using a cell viability assay. One hundred μL media is removed from Each well and replaced with 100 μL of phosphate-buffered saline containing 1.7 mg mL XTT and 5 μg mL PMS. Following 1 hour incubation at 37℃, 20 μL of 2% Triton X- 100 is added to each well and absorbance is read at 450 nM with a background subtraction at 650 nM the data are plotted as cell viability vs. Drug concentration Cell viability is expressed as a percentage o the signal from untreated Samples (0% cytotoxicity) afte the subtraction of signal from Samples treated with 10 μM of Podophyllotoxin (100% cytotoxicity) the CC50 value is calculated fro the Inhibition plots a the concentration of drug which inhibits cell proliferation by 50%.

Storage & Handling

• Storage: store at low temperature,keep away from moisture,store under nitrogen | Pure form: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
• Disclaimer: For research use only

Alternative Names

CYP3A, CYPs, Cytochrome P450, Cobicistat, antiviral, GS 9350, GS9350, GS-9350, Human immunodeficiency virus, HIV, HIV Protease, HIV-1, HIVProtease, inhibit, Inhibitor, Tybost

Compound Identifiers

PubChem CID

25151504