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阿扎那韦硫酸盐 /Atazanavir Sulfate {[allProObj[0].p_purity_real_show]}

货号:A276573 同义名: 硫酸阿扎那韦 / BMS-232632 sulfate;BMS-232632-05

Atazanavir Sulfate is a protease inhibitor used as an antiretroviral medication to treat and prevent HIV/AIDS.

Atazanavir Sulfate 化学结构 CAS号:229975-97-7
Atazanavir Sulfate 化学结构
CAS号:229975-97-7
Atazanavir Sulfate 3D分子结构
CAS号:229975-97-7
Atazanavir Sulfate 化学结构 CAS号:229975-97-7
Atazanavir Sulfate 3D分子结构 CAS号:229975-97-7
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Atazanavir Sulfate 纯度/质量文件 产品仅供科研

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产品名称 HIV Protease HIV-1 caspid 其他靶点 纯度
Dextran sulfate sodium, mw 40,000 M.W 40000
Vicriviroc maleate 98+%
Rosamultin 97%
Darunavir 98%
Lopinavir ++++

HIV protease, Ki: 1.3 pM

99+%
Chloroquine Autophagy 95%
Amprenavir +

HIV protease, IC50: 14.6 ng/mL

PXR 99%+
NBD-556 99%+
Nelfinavir Mesylate +++

HIV protease, Ki: 2 nM

99%+
Atazanavir Sulfate 98%
Limonin 98%
Saquinavir ++

HIV proteinase, IC50: 2.7 nM

98%
Ritonavir 98%
Azvudine 98%
Lenacapavir ++++

HIV-1 capsid, EC50: 0.1 nM

97%
1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多,抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用,但抑制强度暂时没有相关数据。

Atazanavir Sulfate 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.

Atazanavir Sulfate 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 - -

Atazanavir Sulfate 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.

Atazanavir Sulfate 实验方案

计算器
存储液制备 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

Atazanavir Sulfate 技术信息

CAS号229975-97-7
分子式C38H54N6O11S
分子量 802.934
别名 硫酸阿扎那韦 ;BMS-232632 sulfate;BMS-232632-05;Reyataz
运输蓝冰
存储条件

液体 -20°C:3-6个月-80°C:12个月

粉末 Inert atmosphere,2-8°C

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

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