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货号:A100140 同义名: MK 0518 potassium;Raltegravir (potassium salt)

Raltegravir potassium(MK 0518)是一种用于治疗HIV感染的强力整合酶(IN)抑制剂。

Raltegravir potassium 化学结构 CAS号:871038-72-1
Raltegravir potassium 化学结构
CAS号:871038-72-1
Raltegravir potassium 3D分子结构
CAS号:871038-72-1
Raltegravir potassium 化学结构 CAS号:871038-72-1
Raltegravir potassium 3D分子结构 CAS号:871038-72-1
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Raltegravir potassium 纯度/质量文件 产品仅供科研

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Raltegravir potassium 生物活性

描述 Raltegravir potassium is a potent and generally well tolerated integrase (IN) inhibitor, used to treat HIV infection. Raltegravir blocks HIV replication by inhibiting essential strand-transfer activities of integrase[3]. Raltegravir has potent in vitro activity against HIV-1, with a 95% inhibitory concentration of 31±20 nM, in human T lymphoid cell cultures. Raltegravir is also active against HIV-2 when Raltegravir is tested in CEMx174 cells, with an IC95 of 6 nM. Raltegravir metabolism occurs primarily through glucuronidation. Drugs that are strong inducers of the glucuronidation enzyme, UGT1A1, significantly reduce Raltegravir concentrations and should not be used. Raltegravir exhibits weak inhibitory effects on hepatic cytochrome P450 activity. Raltegravir does not induce CYP3A4 RNA expression or CYP3A4-dependent testosterone 6-β-hydroxylase activity[4]. In acutely infected human lymphoid CD4+ T-cell lines MT-4 and CEMx174, SIVmac251 replication is efficiently inhibited by Raltegravir, which shows an EC90 in the low nanomolar range[5].

Raltegravir potassium 临床研究

NCT号 适应症或疾病 临床期 招募状态 预计完成时间 地点
NCT01121809 HIV-1 Infection ... 展开 >> HIV Infections 收起 << Phase 4 Completed - Spain ... 展开 >> Hospitales Universitarios Virgen del Rocio Sevilla, Spain, 41013 收起 <<
NCT00520897 HIV Infections Phase 2 Completed - Canada, Ontario ... 展开 >> Maple Leaf Medical Clinic Toronto, Ontario, Canada, M5B 1L6 收起 <<
NCT00666705 - Completed - -

Raltegravir potassium 参考文献

[1]Hare S, Smith SJ, et al. Structural and functional analyses of the second-generation integrase strand transfer inhibitor dolutegravir (S/GSK1349572). Mol Pharmacol. 2011 Oct;80(4):565-72.

[2]Hare S, Vos AM, et al. Molecular mechanisms of retroviral integrase inhibition and the evolution of viral resistance. Proc Natl Acad Sci U S A. 2010 Nov 16;107(46):20057-62.

[3]Cocohoba J, Dong BJ. Raltegravir: the first HIV integrase inhibitor. Clin Ther. 2008;30(10):1747-1765.

[4]Hicks C, Gulick RM. Raltegravir: the first HIV type 1 integrase inhibitor. Clin Infect Dis. 2009;48(7):931-939. 

[5]Lewis MG, Norelli S, Collins M, et al. Response of a simian immunodeficiency virus (SIVmac251) to raltegravir: a basis for a new treatment for simian AIDS and an animal model for studying lentiviral persistence during antiretroviral therapy. Retrovirology. 2010;7:21

Raltegravir potassium 实验方案

计算器
存储液制备 1mg 5mg 10mg

1 mM

5 mM

10 mM

2.07mL

0.41mL

0.21mL

10.36mL

2.07mL

1.04mL

20.73mL

4.15mL

2.07mL

Raltegravir potassium 技术信息

CAS号871038-72-1
分子式C20H20FKN6O5
分子量 482.507
别名 MK 0518 potassium;Raltegravir (potassium salt);MK-0518
运输蓝冰
存储条件

液体 -20°C:3-6个月-80°C:12个月

粉末 Inert atmosphere,Store in freezer, under -20°C

溶解度

DMSO: 20 mg/mL(41.45 mM),配合低频超声,并水浴加热至45℃助溶,注意:DMSO长时间开封后,会吸水并导致溶解能力下降,请避免使用长期开封的DMSO

H2O: 25 mg/mL(51.81 mM),配合低频超声助溶

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