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Atazanavir sulfate

MCE China：Atazanavir sulfate

Brand：MedChemExpress (MCE)

Cat. No.HY-17367A

CAS：229975-97-7

Synonyms：BMS-232632 sulfate

Purity：99.94%

Storage：4°C, sealed storage, away from moisture *In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

Shipping：Room temperature in continental US; may vary elsewhere.

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.

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].

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].

IC50 & Target：CYP3 HIV-1

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

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References：

[1]. Havlir DV, et al. Atazanavir: new option for treatment of HIV infection. Clin Infect Dis. 2004 Jun 1;38(11):1599-604.  [Content Brief]

[2]. Wood R. Atazanavir: its role in HIV treatment. Expert Rev Anti Infect Ther. 2008 Dec;6(6):785-96.  [Content Brief]

[3]. Qi Sun, et al. Bardoxolone and bardoxolone methyl, two Nrf2 activators in clinical trials, inhibit SARS-CoV-2 replication and its 3C-like protease. Signal Transduct Target Ther. 2021 May 29;6(1):212.  [Content Brief]

[4]. Zhang G, et al. Long-term oral atazanavir attenuates myocardial infarction-induced cardiac fibrosis. Eur J Pharmacol. 2018 Jun 5;828:97-102.  [Content Brief]

[5]. Fukushima K, et al. Effect of serum lipids on the pharmacokinetics of atazanavir in hyperlipidemic rats. Biomed Pharmacother. 2009 Nov;63(9):635-42.  [Content Brief]

[6]. Pyrko P, et al. HIV-1 protease inhibitors nelfinavir and atazanavir induce malignant glioma death by triggering endoplasmic reticulum stress. Cancer Res. 2007 Nov 15;67(22):10920-8.  [Content Brief]

[7]. Alomar FA, et al. Efavirenz, atazanavir, and ritonavir disrupt sarcoplasmic reticulum Ca2+ homeostasis in skeletal muscles. Antiviral Res. 2021 Mar;187:104975.  [Content Brief]

[8]. Robillard KR, et al. Role of P-glycoprotein in the distribution of the HIV protease inhibitor atazanavir in the brain and male genital tract. Antimicrob Agents Chemother. 2014;58(3):1713-22.  [Content Brief]