Atazanavir

Catalog No.S4662 Batch:S466201

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Technical Data

Formula

C38H52N6O7
Molecular Weight 704.86 CAS No. 198904-31-3
Solubility (25°C)* In vitro DMSO 100 mg/mL (141.87 mM)
Ethanol 32 mg/mL (45.39 mM)
Water Insoluble
* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.
* Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.)

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Biological Activity

Description Atazanavir (Latazanavir, Zrivada, Reyataz, BMS-232632) is an azapeptide and HIV-protease inhibitor that is used in the treatment of HIV infections and AIDS in combination with other anti-HIV agents. Atazanavir is a substrate and inhibitor of cytochrome P450 isozyme 3A (CYP3A4) and an inhibitor and inducer of P-glycoprotein.
Targets
HIV protease [1]
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].

Protocol (from reference)

Cell Assay:[3]
  • Cell lines

    The malignant glioma cell lines U251, LN229 and T98G

  • Concentrations

    0-100 μM

  • Incubation Time

    48 h

  • Method

    U251, T98G, 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.
Animal Study:[2]
  • Animal Models

    The WT mice (FVB/NTac strain), TKO mice (FVB/N7 strain)

  • Dosages

    10 mg/kg

  • Administration

    i.v.

Selleck's Atazanavir has been cited by 10 publications

In Vitro Susceptibility of HIV Isolates with High Growth Capability to Antiretroviral Drugs [ Int J Mol Sci, 2022, 23(23)15380] PubMed: 36499705
Going Viral: An Investigation into the Chameleonic Behaviour of Antiviral Compounds [ Chemistry, 2022, e202202798.] PubMed: 36286339
HOPX Plays a Critical Role in Antiretroviral Drugs Induced Epigenetic Modification and Cardiac Hypertrophy [ Cells, 2021, 10(12)3458] PubMed: 34943964
Characterization of fluorescent probe substrates to develop an efficient high-throughput assay for neonatal hepatic CYP3A7 inhibition screening [ Sci Rep, 2021, 11(1):19443] PubMed: 34593846
Antiretroviral Drugs Regulate Epigenetic Modification of Cardiac Cells Through Modulation of H3K9 and H3K27 Acetylation [ Front Cardiovasc Med, 2021, 8:634774] PubMed: 33898535
Altered Gut Microbiome under Antiretroviral Therapy: Impact of Efavirenz and Zidovudine [ ACS Infect Dis, 2020, 10.1021/acsinfecdis.0c00536] PubMed: 33346662
Discovery of M Protease inhibitors encoded by SARS-CoV-2 [ Antimicrob Agents Chemother, 2020, AAC.00872-20] PubMed: 32669265
Calibrating the In Vitro-In Vivo Correlation for OATP-Mediated Drug-Drug Interactions with Rosuvastatin Using Static and PBPK Models [ Drug Metab Dispos, 2020, 48(12):1264-1270] PubMed: 33037044
Selective cell death of latently HIV-infected CD4+ T cells mediated by autosis inducing nanopeptides. [ Cell Death Dis, 2019, 10(6):419] PubMed: 31142734
Co-treatment With HIV Protease Inhibitor Nelfinavir Greatly Increases Late-phase Apoptosis of Drug-resistant KBV20C Cancer Cells Independently of P-Glycoprotein Inhibition. [ Anticancer Res, 2019, 39(7):3757-3765] PubMed: 31262902

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SHIPPING AND STORAGE
Selleck products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Selleck Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Selleck products are stable under the recommended conditions.

NOT FOR HUMAN, VETERINARY DIAGNOSTIC OR THERAPEUTIC USE.