产品说明书

Saquinavir

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Chemical Structure| 127779-20-8 同义名 : Ro 31-8959
CAS号 : 127779-20-8
货号 : A344427
分子式 : C38H50N6O5
纯度 : 98%
分子量 : 670.841
MDL号 : MFCD00866925
存储条件：

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

液体 -20°C:3-6个月-80°C:12个月
溶解度 :

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
动物实验配方：
生物活性
靶点

  • HIV Protease

    HIV proteinase, IC50:2.7 nM
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.
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
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 <<
实验方案
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
参考文献

[1]Momcilović M, Mangano K, et al. Saquinavir-NO inhibits IL-6 production in macrophages. Basic Clin Pharmacol Toxicol. 2014 Dec;115(6):499-506.

[2]Li F, Lu J, et al. CPY3A4-mediated α-hydroxyaldehyde formation in saquinavir metabolism. Drug Metab Dispos. 2014 Feb;42(2):213-20.