Molecular Formula | C38H52N6O7 |
Molar Mass | 704.86 |
Density | 1.178±0.06 g/cm3(Predicted) |
Melting Point | 207-2090C |
Specific Rotation(α) | D -47° (c = 1 in ethanol) |
Solubility | Soluble in methanol, ethanol (~2 mg/ml), DMSO (~16 mg/ml), DMF (~25 mg/ml), and DMF:PBS |
Appearance | Crystalline solid |
Color | white to beige |
pKa | 11.11±0.46(Predicted) |
Storage Condition | -20°C |
Refractive Index | 1.562 |
Use | A highly potent HIV-1 protease inhibitor |
In vitro study | Atazanavir has potent activity against wild-type virus in vitro with EC50 and EC90 at 2-5 nM and 9-15 nM, respectively. Atazanavir can effectively induce endoplasmic reticulum stress response in malignant glioma cells, GRP78 and CHOP levels are increased, caspase-4 is activated, leading to cell death. |
In vivo study | Atazanavir has good oral bioavailability, and its availability is 60-70%. |
overview | azanavir is a new HIV-1 protease inhibitor developed by Bristol-Myers Squibb Company in the United States. Azanavir sulfate was listed in the United States and Europe on June 20, 2003 and March 2, 2004, respectively, under the trade name Ruiyituo (Reyataz). |
Mechanism of action | Azanavir is an azapeptide HIV-1 protease inhibitor. This product selectively inhibits the specific processing process of virus Gag and Gag-Pol poly protein in HIV-1 infected cells, thus blocking the formation of mature virus. In vitro antiviral activity: The average 50% inhibitory concentration (IC50) of azanavir for laboratory and clinical isolates of HIV-1 virus strains implanted in a large number of peripheral blood mononuclear cells, macrophages, CEM-SS cells and MT2 cells without human serum is 2 ~ 5nM. |
biological activity | Atazanavir (Latazanavir, Zrivada, Reyataz, BMS-232632) is an azeptide and HIV-protease inhibitor, often combined with other anti-HIV drugs, Used to treat HIV infection and acquired immune deficiency syndrome. Atazanavir is a substrate and inhibitor of cytochrome P450 isozyme 3A (CYP3A4), as well as an inhibitor and inducer of P-glycoprotein. |
Target | Value |
toxic substance data | information provided by: pubchem.ncbi.nlm.nih.gov (external link) |