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 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.|
|Incubation time||6 days|
|Animal models||male Wistar rats model|
|Formulation||50% ethanol-50% normal saline|
|Administration||constant intravenous infusion|
|Body Surface Area (m2)||0.007||0.025||0.15||0.05||0.02||0.5|
|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.
|Solubility||DMSO 100 mg/mL|
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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