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Atazanavir

Catalog No. T0100L   CAS 198904-31-3
Synonyms: Zrivada, Reyataz, Latazanavir, BMS-232632

Atazanavir (BMS-232632)(BMS-232632) is an highly effective HIV-1 protease inhibitor.

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Atazanavir Chemical Structure
Atazanavir, CAS 198904-31-3
Pack Size Availability Price/USD Quantity
5 mg In stock $ 39.00
10 mg In stock $ 63.00
25 mg In stock $ 96.00
50 mg In stock $ 126.00
100 mg In stock $ 216.00
200 mg In stock $ 323.00
500 mg In stock $ 547.00
1 mL * 10 mM (in DMSO) In stock $ 63.00
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Purity: 99.95%
Purity: 99.76%
Purity: 98%
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Biological Description
Chemical Properties
Storage & Solubility Information
Description Atazanavir (BMS-232632)(BMS-232632) is an highly effective HIV-1 protease inhibitor.
In vitro Atazanavir has potent in vitro activity with 50 and 90% effective concentrations(EC50) of 2-5 nM and 9-15 nM respectively against wild type virus[1]. Atazanavir is able to potently induce endoplasmic reticulum (ER) stress response in malignant glioma cells, as indicated by elevated levels of GRP78 and CHOP, and activation of caspase-4, which leads to cell death[3].
In vivo Atazanavir has excellent oral bioavailability in the range of 60-70%[1].
Kinase Assay Protease assays: To determine the inhibition constants (Ki) for each Prt inhibitor, purified HIV-1 RF wild-type Prt (2.5 nM) is incubated at 37 ℃ with 1 μM to 15 μM fluorogenic substrate in reaction buffer (1 M NaCl, 1 mM EDTA, 0.1 M sodium acetate [pH 5.5], 0.1% polyethylene glycol 8000) in the presence or absence of Atazanavir. Cleavage of the substrate is quantified by measuring an increase in fluorescent emission at 490 nM after excitation at 340 nM using a Cytofluor 4000. Reactions are carried out using 1.36 μM, 1.66 μM, 2.1 μM, 3.0 μM, 5.0 μM, or 15 μM substrate in the presence of five concentrations of Atazanavir (1.25 nM to 25 nM). Substrate cleavage is monitored at 5-min intervals for 30 min. Cleavage rates are then determined for each sample at early time points in the reaction, and Ki values are determined from the slopes of the resulting Michaelis-Menten plots.
Cell Research U251, T98 g, and LN229 glioblastoma cell lines are exposed to increasing concentrations of nelfinavir and atazanavir. Cells cultured in 96-well plates are treated with drugs for 48 h, and cell growth and survival are determined by conventional MTT assay.(Only for Reference)
Synonyms Zrivada, Reyataz, Latazanavir, BMS-232632
Molecular Weight 704.86
Formula C38H52N6O7
CAS No. 198904-31-3

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

Ethanol: 32 mg/mL (45.4 mM)

DMSO: 55 mg/mL (78.03 mM)

H2O: < 1 mg/mL (insoluble or slightly soluble)

TargetMolReferences and Literature

1. Piliero PJ, et al. Expert Opin Investig Drugs. 2002, 11(9):1295-301. 2. Robillard KR, et al. Antimicrob Agents Chemother. 2014, 58(3):1713-22. 3. Pyrko P, et al. Cancer Res. 2007, 67(22):10920-8. 4. Fical L. Vývoj UHPLC-MS/MS metody pro analýzu vybraných antivirotik v HILIC a RP módu[J]. 2020 5. Fical L, Khalikova M, Kočová Vlčková H, et al. Determination of Antiviral Drugs and Their Metabolites Using Micro-Solid Phase Extraction and UHPLC-MS/MS in Reversed-Phase and Hydrophilic Interaction Chromatography Modes[J]. Molecules. 2021, 26(8): 2123.

TargetMolCitations

1. Yan F, Gao F. An overview of potential inhibitors targeting non-structural proteins 3 (PLpro and Mac1) and 5 (3CLpro/Mpro) of SARS-CoV-2. Computational and Structural Biotechnology Journal. 2021, 19: 4868. 2. Fical L, Khalikova M, Kočová Vlčková H, et al. Determination of Antiviral Drugs and Their Metabolites Using Micro-Solid Phase Extraction and UHPLC-MS/MS in Reversed-Phase and Hydrophilic Interaction Chromatography Modes. Molecules. 2021, 26(8): 2123.

Related compound libraries

This product is contained In the following compound libraries:
Drug Repurposing Compound Library Anti-Neurodegenerative Disease Compound Library Anti-Cancer Drug Library Anti-Cancer Clinical Compound Library Membrane Protein-targeted Compound Library EMA Approved Drug Library Inhibitor Library Highly Selective Inhibitor Library Anti-Cancer Approved Drug Library Cardiotoxicity Compound Library

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Keywords

Atazanavir 198904-31-3 Membrane transporter/Ion channel Metabolism Microbiology/Virology Neuroscience Proteases/Proteasome HIV Protease SARS-CoV P450 P-gp CD243 BMS 232632 Pgp Zrivada Cluster of differentiation 243 Reyataz HIV inhibit SARS coronavirus Latazanavir Human immunodeficiency virus Inhibitor P-glycoprotein ABCB1 Cytochrome P450 CYPs MDR1 BMS232632 Multidrug resistance protein 1 BMS-232632 inhibitor

 

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