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Saquinavir
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
Saquinavir图片
CAS NO:127779-20-8
包装与价格:
包装价格(元)
5 mg电议
100 mg电议
1 mL*10 mM(in DMSO)电议

产品名称
沙奎那韦
Ro 31-8959
产品介绍
Saquinavir 是一种 HIV 蛋白酶抑制剂,可研究逆转录病毒。它也是SARS-CoV 3CLpro抑制剂,IC50为 1.36 μM。

产品描述

Saquinavir is a potent HIV protease inhibitor, is an antiretroviral drug used together with other medications to treat or prevent HIV/AIDS.

体内活性

The AUC was not affected by grapefruit juice after intravenous administration, but it increased significantly from 76+/-96 (water, mean (s.d.) to 114+/-70 (microg l[-1] h) (grapefruit juice) after oral saquinavir. Similarly, the oral bioavailability of saquinavir increased by a factor of 2 with grapefruit juice (from 0.7% to 1.4%). In contrast, clearance, volume of distribution and elimination half-life of saquinavir were not affected by grapefruit juice. After oral, but not after intravenous administration, the plasma concentration-time curve showed a second peak after lunch irrespective of pretreatment, suggesting enhancement of absorption by food[1].

动物实验

After an overnight fast, eight healthy volunteers were treated with either 400 ml grapefruit juice or water before intravenous (12 mg) or oral saquinavir (600 mg) was administered.?Serial blood samples were obtained over the following 24 h and standardized meals were served 5 and 10 h after the administration of saquinavir.?The plasma concentrations of saquinavir were determined by high-performance liquid chromatography and pharmacokinetic parameters were calculated by routine methods[1].

Cas No.

127779-20-8

分子式

C38H50N6O5

分子量

670.855

别名

沙奎那韦;Ro 31-8959

储存和溶解度

DMSO:100 mg/mL (149.07 mM)
Powder: -20°C for 3 years
In solvent: -80°C for 2 years