Atazanavir sulfate (BMS-232632, Reyataz) is a sulfate salt form of atazanavir (BMS-232632) that is an highly potent HIV protease inhibitor with EC50 and EC90 of 2.6~5.3 nM and 9~15 nM in cell culture. Atazanavir (BMS-232632) blocks the cleavage of viral precursor proteins in HIV-infected cells. Atazanavir (BMS-232632) is generally more potent than the five currently approved HIV-1 Prt inhibitors. Furthermore, Atazanavir (BMS-232632) is highly selective for HIV-1 Prt and exhibits cytotoxicity only at concentrations 6,500- to 23, 000-fold higher than that required for anti-HIV activity.
Cell Experiment | |
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Cell lines | MT-2 and CEM-SS cells, monocytes/macrophages, and PBMCs |
Preparation method | To determine cytotoxicity, host cells were incubated in the presence of serially diluted inhibitors for 6 days and cell viability was quantitated using an XTT [2,3-bis(2-methoxy-4-nitro-5-sulfophenyl-2H-tetrazolium-5-carboxanilide] assay to calculate the 50% cytotoxic concentrations (CC50s) (42). To assess the effect of human serum proteins on antiviral activity, the 10% fetal calf serum normally used for assays was replaced with 40% adult human serum (Sigma) or 1 mg of α1-acid glycoprotein (Sigma)/ml. |
Concentrations | 0~100 μM |
Incubation time | 6 days |
Animal Experiment | |
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Animal models | male Wistar rats model |
Formulation | 50% ethanol-50% normal saline |
Dosages | 80mg/kg/min |
Administration | constant intravenous infusion |
Molecular Weight | 802.93 |
Formula | C38H52N6O7.H2SO4 |
CAS Number | 229975-97-7 |
Solubility (25°C) | DMSO 100 mg/mL |
Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
Species | Mouse | Rat | Rabbit | Guinea pig | Hamster | Dog |
Weight (kg) | 0.02 | 0.15 | 1.8 | 0.4 | 0.08 | 10 |
Body Surface Area (m2) | 0.007 | 0.025 | 0.15 | 0.05 | 0.02 | 0.5 |
Km factor | 3 | 6 | 12 | 8 | 5 | 20 |
Animal A (mg/kg) = Animal B (mg/kg) multiplied by | Animal B Km |
Animal A Km |
For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.
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