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Atazanavir

Catalog No. T0100L CAS 198904-31-3

Synonyms: Reyataz, Zrivada, BMS-232632, Latazanavir

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

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Atazanavir, CAS 198904-31-3

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Purity: 98%

Biological Description

Chemical Properties

Storage & Solubility Information

Description	Atazanavir(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	Reyataz, Zrivada, BMS-232632, Latazanavir
Molecular Weight	704.87
Formula	C38H52N6O7
CAS No.	198904-31-3

Storage

Powder: -20°C for 3 years

In solvent: -80°C for 2 years

Solubility Information

Ethanol: 32 mg/mL (45.4 mM)

DMSO: 65 mg/mL (92.2 mM)

H2O: <1 mg/mL

( < 1 mg/ml refers to the product slightly soluble or insoluble )

References 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.

Citations

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.

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Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO (Master liquid concentration mg/mL)，Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.

Method for preparing in vivo formulation：Take μL DMSO master liquid, next add μL PEG300， mix and clarify, next add μL Tween 80，mix and clarify, next add μL ddH₂O, mix and clarify.

Note:

Be sure to add the solvent(s) in order. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.

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Tech Support

Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc.

Keywords

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

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