GSK744 (S/GSK1265744)
mRNA synthesis
In vitro transcription of capped mRNA with modified nucleotides and Poly(A) tail
Tyramide Signal Amplification (TSA)
TSA (Tyramide Signal Amplification), used for signal amplification of ISH, IHC and IC etc.
Phos Binding Reagent Acrylamide
Separation of phosphorylated and non-phosphorylated proteins without phospho-specific antibody
Cell Counting Kit-8 (CCK-8)
A convenient and sensitive way for cell proliferation assay and cytotoxicity assay
SYBR Safe DNA Gel Stain
Safe and sensitive stain for visualization of DNA or RNA in agarose or acrylamide gels.
Inhibitor Cocktails
Protect the integrity of proteins from multiple proteases and phosphatases for different applications.
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.
| 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 |
| SDF | Download SDF |
| 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 | 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。 |
| 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 | ||||||
质量控制和MSDS
- 批次:
化学结构
