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Atazanavir Sulfate

Cat. No. M1657
Atazanavir Sulfate Structure
Synonym:

BMS-232632, Reyataz, CGP-73547

Size Price Availability Quantity
10mg USD 100 In stock
50mg USD 250 In stock
100mg USD 350 In stock
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Biological Activity

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.

Protocol
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
Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)
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 resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 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 resveratrol of 11.2 mg/kg.

Chemical Information
Molecular Weight 802.93
Formula C38H52N6O7.H2SO4
CAS Number 229975-97-7
Purity 98.62%
Solubility DMSO 150 mg/mL
Storage at -20°C
References

Mutations selected in HIV-2-infected patients failing a regimen including atazanavir.
Cavaco-Silva et al. J Antimicrob Chemother. 2012 Sep 13. PMID: 22977160.

Atazanavir-based antiretroviral therapy is associated with higher hepatitis C virus viral load in HIV/hepatitis C virus patients.
Rivero-Juarez et al. AIDS Res Hum Retroviruses. 2012 Sep 11. PMID: 22966845.

The protease inhibitor atazanavir triggers autophagy and mitophagy in human preadipocytes.
Gibellini et al. AIDS. 2012 Aug 31. PMID: 22948272.

Duration of first-line antiretroviral therapy with tenofovir and emtricitabine combined with atazanavir/ritonavir, efavirenz or lopinavir/ritonavir in the Italian ARCA cohort.
Di Biagio et al. J Antimicrob Chemother. 2012 Aug 25. PMID: 22915463.

Efficacy and safety of a dual boosted protease inhibitor-based regimen, atazanavir and fosamprenavir/ritonavir, against HIV: experience in a pediatric population.
Rusconi et al. BMC Infect Dis. 2012 Aug 6;12:179. PMID: 22866946.

GS-8374, a novel HIV protease inhibitor, does not alter glucose homeostasis in cultured adipocytes or in a healthy-rodent model system.
Hruz PW, et al. Antimicrob Agents Chemother. 2011 Apr;55(4):1377-82. PMID: 21245443.

BMS-232632, a highly potent human immunodeficiency virus protease inhibitor that can be used in combination with other available antiretroviral agents.
Robinson BS, et al. Antimicrob Agents Chemother. 2000 Aug;44(8):2093-9. PMID: 10898681.

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Keywords: Atazanavir Sulfate, BMS-232632, Reyataz, CGP-73547 supplier, HIV Protease, inhibitors

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