| CAS NO: | 1051375-10-0 |
| 包装 | 价格(元) |
| 10mM (in 1mL DMSO) | 电议 |
| 5mg | 电议 |
| 10mg | 电议 |
| 50mg | 电议 |
| 100mg | 电议 |
| Physical Appearance | A solid |
| Storage | Store at -20°C |
| M.Wt | 405.35 |
| Cas No. | 1051375-10-0 |
| Formula | C19H17F2N3O5 |
| Synonyms | GSK 744;GSK-744 |
| Solubility | insoluble in H2O; insoluble in EtOH; ≥19.35 mg/mL in DMSO with gentle warming |
| Chemical Name | (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 SMILES | FC1=CC(F)=CC=C1CNC(C2=CN(C3=C(C2=O)O)C[C@H]4OC[C@H](C)N4C3=O)=O |
| 运输条件 | 蓝冰运输或根据您的需求运输。 |
| 一般建议 | 为了使其更好的溶解，请用37℃加热试管并在超声波水浴中震动片刻。不同厂家不同批次产品溶解度各有差异，仅做参考。若实验所需浓度过大至产品溶解极限，请添加助溶剂助溶或自行调整浓度。溶液形式一般不宜长期储存，请尽快用完。 |
GSK744 (S/GSK1265744)是一种有效的HIV整合酶抑制剂，IC50值为3 nM[1]。
HIV整合酶是由HIV病毒产生的一种酶，能够使其遗传物质整合到感染细胞的DNA上。据报道，HIV整合酶在抑制HIV的发展中起重要作用[2]。
GSK744 (S/GSK1265744)是一种有效的HIV整合酶抑制剂。在用HIV-1抑制剂及整合酶链转移抑制剂抗性的定点分子（SDM）HIV克隆进行的阻力通道实验、整合酶实验和细胞实验中，GSK1265744通过抑制HIV整合酶，有效抑制HIV的复制[1]。
在阴道内接种猿猴/人类免疫缺陷病毒（一周2次，11周）的雌性猪尾猕猴模型中，GSK744注射可防止猕猴被病毒感染，而对照组在4个中位数的SHIV阴道挑战后被感染，表明GSK744可能是一种潜在的暴露前预防药物，通过抑制HIV整合酶，预防HIV感染[2][3]。
许多已进行的临床试验表明，GSK744可以有效地保护健康受试者免受HIV感染[4-6]。
参考文献：
[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.
| 描述 | GSK744是一种可口服的和长效的HIV整合酶抑制剂。 | |||||
| 靶点 | HIV integrase | |||||
| IC50 | ||||||
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