GSK1349572 sodiuM salt
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.
整合酶抑制剂是一类新的抗逆转录病毒药物,阻断HIV整合酶的活性,而HIV整合酶催化病毒生命周期中的几个关键步骤,对病毒基因组插入到宿主细胞DNA是十分重要的.GSK1349572是下一代HIV整合酶(IN)抑制剂.
体外实验:GSK1349572是双金属结合HIV整合酶链转移的抑制剂,通过阻力通道实验\整合酶实验和机械细胞实验建立了GSK1349572的作用机制及GSK1349572针对其它类抗HIV剂耐受的病毒株的活性.在各种细胞的抗病毒实验中,GSK1349572以亚纳摩尔或低纳摩尔的效力抑制HIV复制,具有9400的选择性指数.外推至100％人血清的蛋白调整半数最大有效浓度为38 nM [1].
在体实验:目前没有可用的动物体内数据.
临床试验:每日服用一次GSK1349572是有效的,没有药代动力学增强,在所有评估剂量下耐受性良好.这些发现支持了每天一次50 mg的GSK1349572的3期临床试验评估.
参考文献：
[1] Kobayashi M, Yoshinaga T, Seki T, Wakasa-Morimoto C, Brown KW, Ferris R, Foster SA, Hazen RJ, Miki S, Suyama-Kagitani A, Kawauchi-Miki S, Taishi T, Kawasuji T, Johns BA, Underwood MR, Garvey EP, Sato A, Fujiwara T. In Vitro antiretroviral properties of S/GSK1349572, a next-generation HIV integrase inhibitor. Antimicrob Agents Chemother. 2011 Feb;55(2):813-21.
[2] van Lunzen J, Maggiolo F, Arribas JR, Rakhmanova A, Yeni P, Young B, Rockstroh JK, Almond S, Song I, Brothers C, Min S. Once daily dolutegravir (S/GSK1349572) in combination therapy in antiretroviral-naive adults with HIV: planned interim 48 week results from SPRING-1, a dose-ranging, randomised, phase 2b trial. Lancet Infect Dis. 2012 Feb;12(2):111-8.
| Physical Appearance | A solid |
| Storage | Store at -20°C |
| M.Wt | 441.36 |
| Cas No. | 1051375-19-9 |
| Formula | C20H18F2N3NaO5 |
| Solubility | insoluble in H2O; insoluble in EtOH; ≥8.06 mg/mL in DMSO with gentle warming |
| Chemical Name | sodium (4R,12aS)-9-((Z)-((2,4-difluorobenzyl)imino)(hydroxy)methyl)-4-methyl-6,8-dioxo-3,4,6,8,12,12a-hexahydro-2H-pyrido[1',2':4,5]pyrazino[2,1-b][1,3]oxazin-7-olate |
| SDF | Download SDF |
| Canonical SMILES | C[C@](N12)([H])CCO[C@@]1([H])CN(C(C2=O)=C3[O-])C=C(/C(O)=N/CC4=C(F)C=C(F)C=C4)C3=O.[Na+] |
| 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。 |
化学结构
