Home Proteases HIV Protease inhibitor - P-gp modulator - P450 (e.g. CYP17) inhibitor Atazanavir For research use only.

Atazanavir

Synonyms: Latazanavir, Zrivada, Reyataz, BMS-232632

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

Atazanavir Chemical Structure

CAS: 198904-31-3

Selleck's Atazanavir has been cited by 9 publications

Purity & Quality Control

Batch: Purity: 99.74%
99.74

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Signaling Pathway

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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
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].
Cell Research 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.
In Vivo
In vivo Atazanavir has excellent oral bioavailability in the range of 60-70%[1].
Animal Research Animal Models The WT mice (FVB/NTac strain), TKO mice (FVB/N7 strain)
Dosages 10 mg/kg
Administration i.v.
NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT04121195 Active not recruiting
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
HIV
St Stephens Aids Trust|Bristol-Myers Squibb
 July 2016 Phase 1

Chemical Information & Solubility

Molecular Weight 704.86 Formula

C38H52N6O7
CAS No. 198904-31-3 SDF Download Atazanavir SDF
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
Storage (From the date of receipt)

In vitro
Batch:

DMSO : 60 mg/mL ( (85.12 mM)； Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Ethanol : 24 mg/mL

Water : Insoluble


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In vivo
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In vivo Formulation Calculator

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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.
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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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