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.
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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。 |
靶点 |
|
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. |
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 | - | - | |
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 |
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 |
动物实验配方 |