2. Anti-infection Metabolic Enzyme/Protease Membrane Transporter/Ion Channel Immunology/Inflammation
  3. HIV HIV Protease SARS-CoV Cytochrome P450 P-glycoprotein Endogenous Metabolite Toll-like Receptor (TLR)
  4. Atazanavir sulfate

Atazanavir sulfate  (Synonyms: BMS-232632 sulfate)

Cat. No.: HY-17367A Purity: 99.94%
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COA
Handling Instructions Technical Support

Atazanavir (BMS-232632) sulfate is a highly selective and orally active HIV-1 protease inhibitor . Atazanavir sulfate is a substrate and inhibitor of CYP3A4, and an inhibitor of P-glycoprotein (P-gp). Atazanavir sulfate is also a SARS-CoV 3CLpro inhibitor with an IC50 of 3.49 μM. Atazanavir sulfate inhibits cardiac fibrosis, hyperlipidemia and induces malignant glioma death.

For research use only. We do not sell to patients.

Atazanavir sulfate Chemical Structure

Atazanavir sulfate Chemical Structure

CAS No. : 229975-97-7

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Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
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Based on 11 publication(s) in Google Scholar

Other Forms of Atazanavir sulfate:

Atazanavir sulfate Related Antibodies

Top Publications Citing Use of Products

View All HIV Isoform Specific Products:

View All Isoforms
HIV HIV-1 HIV-2

View All Cytochrome P450 Isoform Specific Products:

View All Isoforms
CYP1 CYP2 CYP3 CYP4 CYP11 CYP17 Aromatase/CYP19A1 CYP26 CYP51 CYP1A2 CYP2D6 CYP2C9 CYP2C19 CYP3A4 CYP17A1

View All Toll-like Receptor (TLR) Isoform Specific Products:

View All Isoforms
TLR3 TLR8 TLR9 TLR2 TLR4 TLR7 TLR1 TLR6

  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

Atazanavir (BMS-232632) sulfate is a highly selective and orally active HIV-1 protease inhibitor . Atazanavir sulfate is a substrate and inhibitor of CYP3A4, and an inhibitor of P-glycoprotein (P-gp). Atazanavir sulfate is also a SARS-CoV 3CLpro inhibitor with an IC50 of 3.49 μM. Atazanavir sulfate inhibits cardiac fibrosis, hyperlipidemia and induces malignant glioma death[1][2][3][4][5][6][7][8].

IC50 & Target

CYP3

 

HIV-1

 

In Vitro

Atazanavir (1-10 μM, 72 h) attenuates hypoxia induced rat cardiac fibroblasts (rCFs) s proliferation by modulating the HMGB1/TLR 9 pathway[4].
Atazanavir (1-10 μM, 72 h) inhibits collagen I, collagen III, HMGB1, p-IκBα and p-NF-κB expression levels in rat cardiac fibroblasts[4].
Atazanavir (1-10 μM, 48 h) inhibits the growth of A, U251, T98G, LN229 cells and induces ESR (endoplasmic reticulum stress response) in U251, T98G, and LN229 cells[6].
Atazanavir (6.0 μM) elicites Ca2+ transients and blebbing of the plasma membranes of C2C12 skeletal muscle myotubes[7].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Atazanavir sulfate Related Antibodies

Cell Proliferation Assay[4]

Cell Line: Rat cardiac fibroblasts (rCFs)
Concentration: 0, 1, 3, 10 μM
Incubation Time: 72 h
Result: Inhibited rCFs proliferation in a concentration-dependent manner.

Western Blot Analysis[4]

Cell Line: Rat cardiac fibroblasts (rCFs)
Concentration: 0, 1, 3, 10 μM
Incubation Time: 72 h
Result: Reduced collagen I and collagen III levels in a concentration-dependent manner.
Inhibited HMGB1, p-IκBα and p-NF-κB expression.

Cell Viability Assay[6]

Cell Line: A, U251, T98G, LN229 glioblastoma cell
Concentration: 0, 12, 25, 50, 75, 100 μM
Incubation Time: 48 h
Result: Reduced cell growth and survival.

Western Blot Analysis[6]

Cell Line: U251, T98G, and LN229 glioblastoma cell lines
Concentration: 0, 12, 25, 50, 75, 100 μM
Incubation Time: 48 h
Result: Increased GRP78 and CHOP protein levels dose-dependently and activated caspase-4 in all cell lines.
Parmacokinetics
Species Dose Route Indicator value
Rat 7mg/kg i.v. T1/2 1.13hr
Rat 7mg/kg p.o. Cmax 0.54μg/mL
Rat 7mg/kg i.p. T1/2 1.22hr
Rat 7mg/kg i.v. AUC0-∞ 4.09μg·h/mL
Rat 7mg/kg p.o. Tmax 2.25hr
Rat 7mg/kg i.p. AUC0-∞ 3.38μg·h/mL
Rat 7mg/kg i.v. CLtotal 1.77L/h/kg
Rat 7mg/kg p.o. T1/2 1.04hr
Rat 7mg/kg i.v. Vss 2.23L/kg
Rat 7mg/kg p.o. AUC0-∞ 1.70μg·h/mL
In Vivo

Atazanavir (30 mg/kg, i.g., daily, 4 weeks) reduces collagen deposition and inhibits cardiac remodeling in myocardial infarction (MI) model rats[4].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: The myocardial infarction (MI) model was established in adult male Sprague-Dawley rats through surgical procedures[4].
Dosage: 30 mg/kg
Administration: i.g., daily, 4 weeks
Result: Significantly improved systolic pressure (LVSP), +dp/dtmax and −dp/dtmax after MI.
Decreased the non-infarcted LV and hypertrophy of the myocytes.
Significantly attenuated an increase in morphometrical collagen volume fraction in the border left ventricle.
Lowered the heart index (heart-weight to body-weight ratio).
Decreased expressions of α-SMA, HMGB1, TLR 9, p-NF-κB, collagen I and collagen III, and the content of Hyp.
Clinical Trial
Molecular Weight

802.93

Formula

C38H54N6O11S
CAS No.
Appearance

Solid

Color

White to light yellow

SMILES

O=C(OC)N[C@@H](C(C)(C)C)C(NN(CC1=CC=C(C2=NC=CC=C2)C=C1)C[C@H](O)[C@H](CC3=CC=CC=C3)NC([C@H](C(C)(C)C)NC(OC)=O)=O)=O.O=S(O)(O)=O
Structure Classification
Initial Source
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

4°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

Solvent & Solubility
In Vitro: 

DMSO : 166 mg/mL (206.74 mM; Need ultrasonic and warming; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

H2O : < 0.1 mg/mL (insoluble)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.2454 mL 6.2272 mL 12.4544 mL
5 mM 0.2491 mL 1.2454 mL 2.4909 mL
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

  • Molarity Calculator

  • Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass
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Concentration
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Volume
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Molecular Weight *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

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Volume (start)

V1

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Concentration (final)

C2

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Volume (final)

V2

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

  • Protocol 1

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% Saline

    Solubility: ≥ 2.5 mg/mL (3.11 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

    Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
  • Protocol 2

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in Saline)

    Solubility: ≥ 2.5 mg/mL (3.11 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

    Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO +
% 
+
%
Tween-80 +
%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Purity & Documentation

Purity: 99.94%

SDS (580 KB)

COA (255 KB) LCMS (118 KB)

Handling Instructions (2659 KB)
References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 1.2454 mL 6.2272 mL 12.4544 mL 31.1360 mL
5 mM 0.2491 mL 1.2454 mL 2.4909 mL 6.2272 mL
10 mM 0.1245 mL 0.6227 mL 1.2454 mL 3.1136 mL
15 mM 0.0830 mL 0.4151 mL 0.8303 mL 2.0757 mL
20 mM 0.0623 mL 0.3114 mL 0.6227 mL 1.5568 mL
25 mM 0.0498 mL 0.2491 mL 0.4982 mL 1.2454 mL
30 mM 0.0415 mL 0.2076 mL 0.4151 mL 1.0379 mL
40 mM 0.0311 mL 0.1557 mL 0.3114 mL 0.7784 mL
50 mM 0.0249 mL 0.1245 mL 0.2491 mL 0.6227 mL
60 mM 0.0208 mL 0.1038 mL 0.2076 mL 0.5189 mL
80 mM 0.0156 mL 0.0778 mL 0.1557 mL 0.3892 mL
100 mM 0.0125 mL 0.0623 mL 0.1245 mL 0.3114 mL
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Atazanavir sulfate Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

Atazanavir229975-97-7BMS-232632BMS232632BMS 232632HIVHIV ProteaseSARS-CoVCytochrome P450P-glycoproteinEndogenous MetaboliteToll-like Receptor (TLR)Human immunodeficiency virusSARS coronavirusCYPsP-gpPgpMultidrug resistance protein 1MDR1ATP-binding cassette sub-family B member 1ABCB1Cluster of differentiation 243CD243myocardial infarctionserum lipidsgiomaantiviralcardiac fibroblastmyocardial infarction (MI) model ratsα-SMAcollagen Icollagen IIIhyperlipidemicInhibitorinhibitorinhibit

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