| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| 25mg |
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| 50mg |
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| 100mg |
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| 250mg |
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| Other Sizes |
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Purity: ≥98%
Atazanavir Sulfate (also known as Latazanavir, Zrivada, Reyataz, BMS-232632), the sulfate salt form of atazanavir, is a HIV protease inhibitor (PI) for HIV/AIDs treatment with Ki of 2.66 nM in a cell-free assay. The treatment for HIV/AIDS is the same as that of other antiretrovirals. Since it can be given once daily and has less of an impact on the patient's lipid profile than other PIs, atazanavir stands apart from the others. It is used exclusively in conjunction with other HIV medications, similar to other protease inhibitors.
| Targets |
HIV protease (Ki = 2.66 nM)
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| ln Vitro |
Atazanavir has an IC50 of approximately 47 nM for the proteolytic cleavage of the viral gag precursor p55 polyprotein in H9 cells infected with the virus. With an EC50 of 3.89 nM in RF/MT-2 strains, atazanavir demonstrates strong antiviral activity.[1] It is demonstrated that atazanavir inhibits bilirubin glucuronidation with an IC50 of 2.4 μM. Atazanavir has a Ki of 1.9 μM, which inhibits recombinant UGT1A1.[2] In U251, T98G, and LN229 glioblastoma cell lines, atazanavir inhibits cell growth with notably elevated levels of GRP78 and CHOP protein. In U251 glioblastoma cells, atazanavir induces a significant upregulation of polyubiquitinated proteins of diverse sizes.[3] With an IC50 of 26 μM, atazanavir also inhibits the human 20S proteasome. In HepG2 cells, atazanavir (30 μM) modifies the levels of ER stress and UPR gene expression.[4] In LS180V cells, atazanavir (30 mM) results in a 2.5-fold increase in immunoreactive P-gp expression and a decrease in intracellular Rh123.[5]
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| ln Vivo |
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| Enzyme Assay |
Purified HIV-1 RF wild-type Prt (2.5 nM) is incubated at 37 °C with 1 μM to 15 μM fluorogenic substrate in reaction buffer (1 M NaCl, 1 mM EDTA, 0.1 M sodium acetate [pH 5.5], 0.1% polyethylene glycol 8000) with or without atazanavir in order to calculate the inhibition constants (Ki) for each Prt inhibitor. Using a Cytofluor 4000, cleavage of the substrate is measured as an increase in fluorescent emission at 490 nM following excitation at 340 nM. In five different concentrations of Atazanavir (1.25 nM to 25 nM), reactions are conducted with substrate that is 1.36 μM, 1.66 μM, 2.1 μM, 3.0 μM, 5.0 μM, or 15 μM. During a half-hour, the substrate cleavage is observed every five minutes. Then, at early stages of the reaction, cleavage rates are calculated for each sample, and Ki values are ascertained from the slopes of the ensuing Michaelis-Menten plots.
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| Cell Assay |
In order to assess cytotoxicity, host cells are cultured for six days with serially diluted Atazanavir. Cell viability is then measured using the XTT[2,3-bis(2-methoxy-4-nitro-5-sulfophenyl-2H-tetrazolium-5-carboxanilide)] assay, which yields the 50% cytotoxic concentrations (CC50s). In order to evaluate how human serum proteins affect antiviral activity, 40% adult human serum or 1 mg of α1-acid glycoprotein/mL is added to the 10% fetal calf serum that is typically used for assays.
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| Animal Protocol |
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| References |
| Molecular Formula |
C38H54N6O11S
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| Molecular Weight |
802.93
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| Elemental Analysis |
C, 56.84; H, 6.78; N, 10.47; O, 21.92; S, 3.99
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| CAS # |
229975-97-7
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| Related CAS # |
Atazanavir;198904-31-3
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| Appearance |
Solid powder
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| SMILES |
CC(C)(C)[C@@H](C(=O)N[C@@H](CC1=CC=CC=C1)[C@H](CN(CC2=CC=C(C=C2)C3=CC=CC=N3)NC(=O)[C@H](C(C)(C)C)NC(=O)OC)O)NC(=O)OC.OS(=O)(=O)O
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| InChi Key |
DQSGVVGOPRWTKI-QVFAWCHISA-N
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| InChi Code |
InChI=1S/C38H52N6O7.H2O4S/c1-37(2,3)31(41-35(48)50-7)33(46)40-29(22-25-14-10-9-11-15-25)30(45)24-44(43-34(47)32(38(4,5)6)42-36(49)51-8)23-26-17-19-27(20-18-26)28-16-12-13-21-39-28;1-5(2,3)4/h9-21,29-32,45H,22-24H2,1-8H3,(H,40,46)(H,41,48)(H,42,49)(H,43,47);(H2,1,2,3,4)/t29-,30-,31+,32+;/m0./s1
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| Chemical Name |
methyl N-[(2S)-1-[2-[(2S,3S)-2-hydroxy-3-[[(2S)-2-(methoxycarbonylamino)-3,3-dimethylbutanoyl]amino]-4-phenylbutyl]-2-[(4-pyridin-2-ylphenyl)methyl]hydrazinyl]-3,3-dimethyl-1-oxobutan-2-yl]carbamate;sulfuric acid
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| Synonyms |
Atazanavir sulfate; BMS-232632; BMS 232632; BMS232632
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| HS Tariff Code |
2934.99.03.00
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (3.11 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.5 mg/mL (3.11 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.5 mg/mL (3.11 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. Solubility in Formulation 4: ≥ 2.5 mg/mL (3.11 mM) (saturation unknown) in 5% DMSO + 40% PEG300 + 5% Tween80 + 50% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 5: ≥ 2.5 mg/mL (3.11 mM) (saturation unknown) in 5% DMSO + 95% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. Solubility in Formulation 6: 30% PEG400+0.5% Tween80+5% propylene glycol: 30 mg/mL |
| Preparing Stock Solutions | 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 | |
| 10 mM | 0.1245 mL | 0.6227 mL | 1.2454 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution 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 stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
| NCT Number | Recruitment | interventions | Conditions | Sponsor/Collaborators | Start Date | Phases |
| NCT04468087 | Active Recruiting |
Drug: Atazanavir Drug: Daclatasvir 60 mg |
COVID-19 | Hospital do Coracao | February 15, 2021 | Phase 2 Phase 3 |
| NCT04121195 | Active Recruiting |
Drug: Dose escalation | HIV/AIDS Tuberculosis |
University of Liverpool | October 30, 2020 | Phase 2 Phase 3 |
| NCT02016924 | Recruiting | Drug: ATV Drug: DRV |
Acquired Immune Deficiency Syndrome (AIDS) HIV Infections |
Gilead Sciences | January 16, 2014 | Phase 2 Phase 3 |
| NCT04452565 | Recruiting | Drug: Drug: NA-831 Combination Product: NA-831 and Atazanavir |
Coronavirus Infection Severe Acute Respiratory Infection |
NeuroActiva, Inc. | June 15, 2022 | Phase 2 Phase 3 |
| NCT01837719 | Completed | Drug: Atazanavir Drug: Cobicistat |
HIV-1 | Bristol-Myers Squibb | April 2013 | Phase 1 |
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