Atazanavir sulfateAtazanavir sulfate
MedChemExpress (MCE)
HY-17367A
229975-97-7
BMS-232632 sulfate
99.94%
4°C, sealed storage, away from moisture *In solvent : -80°C, 6 months
-20°C, 1 month (sealed storage, away from moisture)
Room temperature in continental US
may vary elsewhere.
Atazanavir (BMS-232632) sulfate is a highly selective and orally active HIV-1 protease inhibitor . Atazanavir sulfate is a substrate and inhibitor of CYP3A4, and an inhibitor of P-glycoprotein (P-gp). Atazanavir sulfate is also a SARS-CoV 3CLpro inhibitor with an IC50 of 3.49 μM. Atazanavir sulfate inhibits cardiac fibrosis, hyperlipidemia and induces malignant glioma death.
Atazanavir (1-10 μM, 72 h) attenuates hypoxia induced rat cardiac fibroblasts (rCFs) s proliferation by modulating the HMGB1/TLR 9 pathway[4]. Atazanavir (1-10 μM, 72 h) inhibits collagen I, collagen III, HMGB1, p-IκBα and p-NF-κB expression levels in rat cardiac fibroblasts[4]. Atazanavir (1-10 μM, 48 h) inhibits the growth of A, U251, T98G, LN229 cells and induces ESR (endoplasmic reticulum stress response) in U251, T98G, and LN229 cells[6]. Atazanavir (6.0 μM) elicites Ca2+ transients and blebbing of the plasma membranes of C2C12 skeletal muscle myotubes[7].
Atazanavir (30 mg/kg, i.g., daily, 4 weeks) reduces collagen deposition and inhibits cardiac remodeling in myocardial infarction (MI) model rats[4].
CYP3 HIV-1
Dose Route Indicator value Rat 7mg/kg i.v. T1/2 1.13hr Rat 7mg/kg p.o. Cmax 0.54μg/mL Rat 7mg/kg i.p. T1/2 1.22hr Rat 7mg/kg i.v. AUC0-∞ 4.09μg·h/mL Rat 7mg/kg p.o. Tmax 2.25hr Rat 7mg/kg i.p. AUC0-∞ 3.38μg·h/mL Rat 7mg/kg i.v. CLtotal 1.77L/h/kg Rat 7mg/kg p.o. T1/2 1.04hr Rat 7mg/kg i.v. Vss 2.23L/kg Rat 7mg/kg p.o. AUC0-∞ 1.70μg·h/mL
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