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阿扎那韦 /Atazanavir {[allProObj[0].p_purity_real_show]}

货号:A182779 同义名: BMS-232632;CGP 73547

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

Atazanavir 化学结构 CAS号:198904-31-3
Atazanavir 化学结构
CAS号:198904-31-3
Atazanavir 3D分子结构
CAS号:198904-31-3
Atazanavir 化学结构 CAS号:198904-31-3
Atazanavir 3D分子结构 CAS号:198904-31-3
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Atazanavir 纯度/质量文件 产品仅供科研

货号:A182779 标准纯度: {[allProObj[0].p_purity_real_show]}
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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 生物活性

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]. The use of HIV protease inhibitors for the treatment of HIV infection remains a primary and effective component of combination antiretroviral therapy. 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]. In a phase I clinical trial of atazanavir, single oral doses of 100, 300, 600, 900 or 1200 mg were given to healthy volunteers, pharmcokinetic profile showed that atazanavir had good oral bioavailability and that peak concentrations and area under the curve increased in a greater-than-dose proportional manner[4]. In a phase II study, atazanavir 400 or 600 mg o.d combined with saquinavir-sgc 1200 mg o.d were compared to ritonavir 400 mg plus saquinavir-sgc 400 mg both twice-daily, at the end of 48 weeks, all 3 arms showed similar declines in viral load (range: 1.19 - 1.6 log10) and increases in CD4 cell counts[4]. Atazanavir significantly attenuated CoCl2-induced neonatal rat cardiac fibroblast (rCFs) proliferation in a concentration-dependent manner[5]. Recently, Atazanavir is undergoing clinical trial for 2019-novel coronavirus treatment.

Atazanavir 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
NCT00544128 HIV Infections Phase 4 Completed - Japan ... 展开 >> International Medical Center of Japan Shinjuku, Tokyo, Japan, 1628655 收起 <<
NCT01105611 HIV Infections ... 展开 >> Hepatitis C 收起 << Phase 4 Unknown December 2012 Ireland ... 展开 >> Department of Genitourinary Medicine and Infectious Diseases, St. James's Hospital Recruiting Dublin, Ireland Contact: Colm Bergin, MD, FRCPI    +35314162507    cbergin@stjames.ie    Contact: James Woo, MB, MRCPI    +353868108086    wooj@tcd.ie    Principal Investigator: Colm Bergin, MD, FRCPI          Sub-Investigator: James Woo, MB, MRCPI          Mater Misericordiae University Hospital Not yet recruiting Dublin, Ireland Contact: Patrick Mallon, MB FRCPI PhD    +35317166311    Paddy.Mallon@ucd.ie    Principal Investigator: Patrick Mallon, MB FRCPI PhD 收起 <<
NCT01458769 Healthy Volunteers Phase 1 Completed - -

Atazanavir 参考文献

[1]Robillard KR, Chan GN, 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.

[2]Piliero PJ. Atazanavir: a novel HIV-1 protease inhibitor. Expert Opin Investig Drugs. 2002 Sep;11(9):1295-301.

[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]Piliero PJ. Atazanavir: a novel HIV-1 protease inhibitor. Expert Opin Investig Drugs. 2002 Sep;11(9):1295-301. doi: 10.1517/13543784.11.9.1295. PMID: 12225250.

[5]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 实验方案

计算器
存储液制备 1mg 5mg 10mg

1 mM

5 mM

10 mM

1.42mL

0.28mL

0.14mL

7.09mL

1.42mL

0.71mL

14.19mL

2.84mL

1.42mL

Atazanavir 技术信息

CAS号198904-31-3
分子式C38H52N6O7
分子量 704.856
别名 BMS-232632;CGP 73547;Reyataz;Zrivada;Latazanavir
运输蓝冰
存储条件

液体 -20°C:3-6个月-80°C:12个月

粉末 Sealed in dry,Store in freezer, under -20°C

溶解度

DMSO: 85 mg/mL(120.59 mM),配合低频超声助溶,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
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