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AtazanavirHIV protease inhibitor,highly potent

Atazanavir

Catalog No. A8205
Size Price Stock Qty
10mM (in 1mL DMSO) $160.00 In stock
Evaluation Sample $28.00 In stock
5mg $70.00 In stock
10mg $100.00 In stock
25mg $160.00 In stock
50mg $250.00 In stock

Tel: +1-832-696-8203

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Sample solution is provided at 25 µL, 10mM.

Product Citations

1. Lan, Jie, et al. "Provirus Activation Plus CD59 Blockage Triggers Antibody-Dependent Complement-Mediated Lysis of Latently HIV-1–Infected Cells." The Journal of Immunology (2014): 1303030. PMID:25149467

Biological Activity

Description Atazanavir is an inhibitor of HIV protease with Ki of 2.66 nM.
Targets HIV          
IC50 2.6~5.3 nM          

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Chemical Properties

Cas No. 198904-31-3 SDF Download SDF
Chemical Name methyl N-[(2S)-1-[2-[(2S,3S)-2-hydroxy-3-[[(2S)-2-(methoxycarbonylamino)-3,3-dimethylbutanoyl]amino]-4-phenylbutyl]-2-[(4-pyridin-2-ylphenyl)methyl]hydrazinyl]-3,3-dimethyl-1-oxobutan-2-yl]carbamate
Canonical SMILES CC(C)(C)C(C(=O)NC(CC1=CC=CC=C1)C(CN(CC2=CC=C(C=C2)C3=CC=CC=N3)NC(=O)C(C(C)(C)C)NC(=O)OC)O)NC(=O)OC
Formula C38H52N6O7 M.Wt 704.9
Solubility >28.6mg/mL in DMSO Storage Store at -20°C
General tips N/A
Shipping Condition N/A

Background

Atazanavir is a novel and potent azapeptide protease inhibitor that specifically inhibits the human immunodeficiency virus type 1 (HIV-1) protease enzyme with inhibition constant Ki of 66 nmol/L and also inhibits the viral replication of HIV-1 with 50% effective concentration EC50 ranging from 2.6 to 5.3 nmol/L. Atazanavir binds to HIV-1 protease preventing the cleavage of gag and gag-pol polyproteins, which results in the formation of immature virions in HIV-1-infected cells. Atazanavir has a different C-2 symmetric chemical structure and a generally greater antiretroviral potency in various HIV strains compared to other protease inhibitors, including indinavir, nelfinavir, ritonavir, saquinavir and amprenavir.

Reference

Fuster D, Clotet B. Review of atazanavir: a novel HIV protease inhibitor. Expert Opin Pharmacother. 2005 Aug;6(9):1565-72.

Croom KF, Dhillon S, Keam SJ. Atazanavir: a review of its use in the management of HIV-1 infection. Drugs. 2009 May 29;69(8):1107-40. doi: 10.2165/00003495-200969080-00009.