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Atazanavir Sulfate

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Chemical Structure| 229975-97-7 同义名 : 硫酸阿扎那韦 ;BMS-232632 sulfate;BMS-232632-05;Reyataz
CAS号 : 229975-97-7
货号 : A276573
分子式 : C38H54N6O11S
纯度 : 98%
分子量 : 802.934
MDL号 : MFCD08067748
存储条件：

粉末 Inert atmosphere,2-8°C

液体 -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 160 mg/mL(199.27 mM)，配合低频超声，并水浴加热至45℃助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO
动物实验配方：
生物活性
靶点

  • HIV Protease

    HIV protease, Ki:2.66 nM

  • HIV Protease
描述 Human immunodeficiency virus type 1 (HIV-1) protease specifically processes gag (p55) and gag-pol (p160) viral polyproteins to yield the viral structural proteins (p17, p24, p7, and p6)[3]. Atazanavir Sulfate (BMS-232632 Sulfate) is a protease inhibitor used to treat and prevent HIV/AIDS. Atazanavir is an azapeptide HIV-1 protease inhibitor that exhibits potent anti-HIV activity with EC50 of 2.6 to 5.3 nM and EC90 of 9 to 15 nM in cell culture[3]. Atazanavir/ritonavir (300/100 mg once daily) inhibited glucose uptake in vitro significantly less than lopinavir/ritonavir (400/100 mg twice daily) for 10 day[4]. In clinical trial, mean reductions from baseline in plasma HIV RNA levels in antiretroviral therapy-naive patients were not significantly different between once-daily atazanavir 400mg and two- or three-times daily nelfinavi or once-daily efavirenz[5]. After 21 days of treatment with atazanavir sulfate plus ritonavir (30 + 10 mg/kg) in Bleomycin (BLM)-induced pulmonary fibrosis model, the BLM-induced pathology score was reduced by 51.0%, and increase in collagen contents and Hyp content were also decreased compared with the BLM group[6]. In myocardial infarction (MI)-induced cardiac fibrosis rats, intragastric administration of atazanavir sulfate 30 mg/k ameliorated changes in the left ventricular systolic pressure (LVSP), + dp/dtmax, and - dp/dtmax after 4 weeks[7]. Recently, it is reported that Atazanavir showed anti-2019-novel coronavirus activity.
临床研究
NCT号 适应症或疾病 临床期 招募状态 预计完成时间 地点
NCT01003990 HIV Phase 3 Completed - -
NCT01591850 Healthy Volunteer Phase 1 Completed - United States, Florida ... 展开 >> Merritt Island, Florida, United States, 32953 收起 <<
NCT01003990 - Completed - -
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

1.25mL

0.25mL

0.12mL

6.23mL

1.25mL

0.62mL

12.45mL

2.49mL

1.25mL
参考文献

[1]Zhang D, Chando TJ, et al. In vitro inhibition of UDP glucuronosyltransferases by atazanavir and other HIV protease inhibitors and the relationship of this property to in vivo bilirubin glucuronidation. Drug Metab Dispos. 2005 Nov;33(11):1729-39.

[2]Robinson BS, Riccardi KA, et al. BMS-232632, a highly potent human immunodeficiency virus protease inhibitor that can be used in combination with other available antiretroviral agents. Antimicrob Agents Chemother. 2000 Aug;44(8):2093-9.

[3]Robinson BS, Riccardi KA, Gong YF, Guo Q, Stock DA, Blair WS, Terry BJ, Deminie CA, Djang F, Colonno RJ, Lin PF. BMS-232632, a highly potent human immunodeficiency virus protease inhibitor that can be used in combination with other available antiretroviral agents. Antimicrob Agents Chemother. 2000 Aug;44(8):2093-9. doi: 10.1128/AAC.44.8.2093-2099.2000. PMID: 10898681; PMCID: PMC90019.

[4]Noor MA, Flint OP, Maa JF, Parker RA. Effects of atazanavir/ritonavir and lopinavir/ritonavir on glucose uptake and insulin sensitivity: demonstrable differences in vitro and clinically. AIDS. 2006 Sep 11;20(14):1813-21. doi: 10.1097/01.aids.0000244200.11006.55. PMID: 16954722.

[5]Croom KF, Dhillon S, Keam SJ. Atazanavir: a review of its use in the management of HIV-1 infection. Drugs. 2009 May 29;69(8):1107-40. doi: 10.2165/00003495-200969080-00009. PMID: 19496633.

[6]Song S, Ji Y, Zhang G, Zhang X, Li B, Li D, Jiang W. Protective Effect of Atazanavir Sulphate Against Pulmonary Fibrosis In Vivo and In Vitro. Basic Clin Pharmacol Toxicol. 2018 Feb;122(2):199-207. doi: 10.1111/bcpt.12871. Epub 2017 Sep 6. PMID: 28816009.

[7]Zhang G, Zhang X, Li D, Tian J, Jiang W. Long-term oral atazanavir attenuates myocardial infarction-induced cardiac fibrosis. Eur J Pharmacol. 2018 Jun 5;828:97-102. doi: 10.1016/j.ejphar.2018.03.041. Epub 2018 Mar 29. PMID: 29605419.