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GSK744(S/GSK1265744)
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。
GSK744(S/GSK1265744)图片
CAS NO:1051375-10-0
包装与价格：
包装价格(元)
10mM (in 1mL DMSO)电议
5mg电议
10mg电议
50mg电议
100mg电议

产品介绍
GSK744 (S/GSK1265744) (GSK-1265744) 是一种具有口服活性的长效 HIV 整合酶抑制剂和有机阴离子转运蛋白 1/3 (OAT1/OAT3) 抑制剂，IC50 值为 2.5 nM, 0.41 μM 和 0.81 ⋼ M 分别代表 HIVADA、OAT3 和 OAT1。
Cas No.1051375-10-0
别名卡博特韦; GSK-1265744; S/GSK1265744
化学名(3S,11aR)-N-(2,4-difluorobenzyl)-6-hydroxy-3-methyl-5,7-dioxo-2,3,5,7,11,11a-hexahydrooxazolo[3,2-a]pyrido[1,2-d]pyrazine-8-carboxamide
Canonical SMILESFC1=CC(F)=CC=C1CNC(C2=CN(C3=C(C2=O)O)C[C@H]4OC[C@H](C)N4C3=O)=O
分子式C19H17F2N3O5
分子量405.35
溶解度≥ 19.35mg/mL in DMSO with gentle warming
储存条件Store at -20℃
General tipsFor obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.
Shipping ConditionEvaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request
产品描述

GSK744 (S/GSK1265744) is a potential inhibitor of HIV integrase with IC50 value of 3 nM [1].
HIV integrase is an enzyme produced by HIV virus that enables its genetic material to be integrated into the infected cell DNA. It is reported that HIV intergrase inhibitor plays an important role in halting HIV progression [2].
GSK744 (S/GSK1265744) is a potent HIV integrase inhibitor. Using resistance passage experiments, integrase enzyme assays, and cellular assays with site-directed molecular (SDM) HIV clones resistant to other classes of anti-HIV-1 agents and earlier integrase strand transfer inhibitors, results showed that GSK1265744 efficiently inhibited HIV replication through inhibiting HIV integrase [1].
In female pigtail macaques model that intravaginal inoculated simian/human immunodeficiency virus twice a week for up to 11 weeks, GSK744 injection prevented the macaques from being infected by virus while placebo controls were infected after a 4 median vaginal challenges with SHIV which reminded that GSK744 may be a potential preexposure prophylaxis drug for prevention via inhibiting HIV integrase [3] [2].
Many clinical trials have been conducted to show that GSK744 can efficiently protected healthy subjects from HIV infection [4-6].
References:
[1].    Yoshinaga, T., et al., Antiviral characteristics of GSK1265744, an HIV integrase inhibitor dosed orally or by long-acting injection. Antimicrob Agents Chemother, 2015. 59(1): p. 397-406.
[2].    Andrews, C.D., et al., Long-acting integrase inhibitor protects macaques from intrarectal simian/human immunodeficiency virus. Science, 2014. 343(6175): p. 1151-4.
[3].    Radzio, J., et al., The long-acting integrase inhibitor GSK744 protects macaques from repeated intravaginal SHIV challenge. Sci Transl Med, 2015. 7(270): p. 270ra5.
[4].    Ford, S.L., et al., Lack of pharmacokinetic interaction between rilpivirine and integrase inhibitors dolutegravir and GSK1265744. Antimicrob Agents Chemother, 2013. 57(11): p. 5472-7.
[5].    Spreen, W., et al., Pharmacokinetics, safety, and tolerability with repeat doses of GSK1265744 and rilpivirine (TMC278) long-acting nanosuspensions in healthy adults. J Acquir Immune Defic Syndr, 2014. 67(5): p. 487-92.
[6].    Spreen, W.R., D.A. Margolis, and J.C. Pottage, Jr., Long-acting injectable antiretrovirals for HIV treatment and prevention. Curr Opin HIV AIDS, 2013. 8(6): p. 565-71.