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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 | |
|---|---|
| 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 | |
|---|---|
| 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 |
| Related HIV Protease Products |
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Arg-Val-(Nle-p-nitro)-Phe-Glu-Ala-Nle-NH2 is a fluorogenic substrate of HIV-1 protease. |
| Ac-Ser-Gln-Asn-Tyr-Pro-Val-Val-NH2
Ac-Ser-Gln-Asn-Tyr-Pro-Val-Val-NH2 is a substrato peptídico of HIV-1 protease. |
| HIV-1, HIV-2 Protease Substrate
HIV-1, HIV-2 Protease Substrate is the substrate of HIV-1, HIV-2 protease. |
| HIV Protease Substrate IV
HIV Protease Substrate IV is a substrate of HIV protease. |
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