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Atazanavir HIV Protease inhibitor

Name: Atazanavir
Brand: Selleck Chemicals
SKU: S4662
Availability: InStock
Rating: 5 (11 reviews)

Cat.No.S4662

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. This compound is a substrate and inhibitor of cytochrome P450 isozyme 3A (CYP3A4) and an inhibitor and inducer of P-glycoprotein.

Chemical Structure

Molecular Weight: 704.86

Jump to Mechanism of Action Solubility Chemical Information, Storage & Stability Specificity

Quality Control

Batch: Purity: 99.74%

99.74

Related Targets	HDAC Caspase MMP HCV Protease Cysteine Protease DPP Tyrosinase Proteasome Serine Protease Secretase PCSK9 Glutaminase Acyltransferase Thrombin Cathepsin B MALT PAD PREP Neprilysin Carboxypeptidase SGK Aminopeptidase 3C-Like Protease PSMA PGDS GOT
Related Products	Pepstatin A Limonin Temsavir (BMS-626529) Rosamultin Bevirimat Dextran sulfate sodium (DSS) Mericitabine NBD-556 GS-6207 Azvudine

Chemical Information, Storage & Stability

Molecular Weight	704.86	Formula	C₃₈H₅₂N₆O₇	Storage (From the date of receipt)	3 years-20°Cpowder
CAS No.	198904-31-3	Download SDF		Storage of Stock Solutions	1 year-80°Cin solvent 1 month-20°Cin solvent
Synonyms	Latazanavir, Zrivada, Reyataz, BMS-232632			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

Solubility

In vitro
Batch:

DMSO : 60 mg/mL (85.12 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Ethanol : 24 mg/mL

Water : Insoluble

Molarity Calculator

Mass	Concentration	Volume	Molecular Weight
Mass value Mass unit	Concentration value Concentration unit	Volume value Volume unit	Molecular weight (g/mol)

Dilution Calculator Molecular Weight Calculator

In vivo batch selection In vivo Batch:
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Clear solution	5%DMSO 1 40%PEG300 2 5%Tween80 3 50%ddH2O Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	3mg/ml (4.26mM)	Taking the 1 mL working solution as an example, add 50 μL of 60 mg/ml clarified DMSO stock solution to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to clarify; then continue to add 500 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results.
Clear solution	5% DMSO 1 95% Corn oil Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	0.43mg/ml (0.61mM)	Taking the 1 mL working solution as an example, add 50 μL of 8.6 mg/ml clear DMSO stock solution to 950 μL of corn oil and mix evenly. The mixed solution should be used immediately for optimal results.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.

In vivo Formulation Calculator (Clear solution)

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

Dosage: mg/kg

Average weight of animals: g

Dosing volume per animal: μL

Number of animals:

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.

Mechanism of Action

Targets/IC₅₀/Ki	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]. This compound 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].
References	[1] https://pubmed.ncbi.nlm.nih.gov/12225250/ [2] https://pubmed.ncbi.nlm.nih.gov/24379203/ [3] https://pubmed.ncbi.nlm.nih.gov/18006837/

Clinical Trial Information

(data from https://clinicaltrials.gov, updated on 2024-05-22)

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

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