Atazanavir

Catalog No.S4662 Synonyms: Latazanavir, Zrivada, Reyataz, BMS-232632

For research use only.

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.

Atazanavir Chemical Structure

CAS No. 198904-31-3

Selleck's Atazanavir has been cited by 7 Publications

Purity & Quality Control

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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 Research:[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.
  • (Only for Reference)
Animal Research:[2]
  • Animal Models: The WT mice (FVB/NTac strain), TKO mice (FVB/N7 strain)
  • Dosages: 10 mg/kg
  • Administration: i.v.
  • (Only for Reference)

Solubility (25°C)

In vitro

DMSO 71 mg/mL
(100.72 mM)
Ethanol 32 mg/mL
(45.39 mM)
Water 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.

Chemical Information

Molecular Weight 704.86
Formula

C38H52N6O7

CAS No. 198904-31-3
Storage 3 years -20°C powder
2 years -80°C in solvent
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

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

mg/kg g μL

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO % % Tween 80 % ddH2O
%DMSO %

Calculation results:

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 addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Molarity Calculator

Mass Concentration Volume Molecular Weight

Clinical Trial Information

NCT Number Recruitment Interventions Conditions Sponsor/Collaborators Start Date Phases
NCT04121195 Recruiting Drug: Dose escalation HIV/AIDS|Tuberculosis University of Liverpool|European and Developing Countries Clinical Trials Partnership (Funder)|Joint Clinical Research Centre Kampala Uganda|University of Cape Town Cape Town South Africa|Infectious Diseases Institute Makerere University College of Health Sciences Kampala Uganda|University of Turin Turin Italy October 30 2020 Phase 2|Phase 3
NCT02697851 Terminated Drug: Microgynon 30®|Drug: Evotaz® HIV St Stephens Aids Trust|Bristol-Myers Squibb July 2016 Phase 1

(data from https://clinicaltrials.gov, updated on 2022-01-17)

Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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