Saquinavir是一种 HIV 蛋白酶抑制剂,常用于抗逆转录病毒治疗。Saquinavir 也能抑制 SARS-CoV-2 3CLpro 主蛋白酶。
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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 | Saquinavir is an orally active and selective HIV proteinase inhibitor. It was highly active against HIV in human cells that are acutely or chronically infected with the virus in in vitro study. Saquinavir had IC50 and IC90 values ranged from 1-30nM and 5-80nM, respectively. Recent study found that Saquinavir showed inhibition effect on 2019-nCoV. |
作用机制 | Saquinavir is a peptide-like substrate analogue that inhibits HIV protease, which is required for the cleavage of viral polyprotein precursor into individual functional proteins as found in infectious HIV, by binding to its active site. Inhibition of HIV protease leads to the production of immature non-infectious virus particles. |
NCT号 | 适应症或疾病 | 临床期 | 招募状态 | 预计完成时间 | 地点 |
NCT01936870 | - | Completed | - | - | |
NCT01936870 | - | Completed | - | - | |
NCT02556268 | HIV-DDI | Phase 1 | Completed | - | United States, Florida ... 展开 >> Orlando, Florida, United States, 32803 United States, Massachusetts Boston, Massachusetts, United States, 02118 收起 << |
计算器 | ||||
存储液制备 | 1mg | 5mg | 10mg | |
1 mM 5 mM 10 mM |
1.49mL 0.30mL 0.15mL |
7.45mL 1.49mL 0.75mL |
14.91mL 2.98mL 1.49mL |
CAS号 | 127779-20-8 |
分子式 | C38H50N6O5 |
分子量 | 670.841 |
别名 | Ro 31-8959 |
运输 | 蓝冰 |
存储条件 |
In solvent -20°C:3-6个月-80°C:12个月 Pure form Sealed in dry,Store in freezer, under -20°C |
溶解方案 |
DMSO: 105 mg/mL(156.52 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 以下溶解方案都请先按照体外实验的方式配制澄清的储备液,再依次添加助溶剂: ——为保证实验结果的可靠性,澄清的储备液可以根据储存条件,适当保存;体内实验的工作液,建议现用现配,当天使用; 以下溶剂前显示的百分比是指该溶剂在终溶液中的体积占比;如在配制过程中出现沉淀、析出现象,可以通过加热和/或超声的方式助溶
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动物实验配方 |