产品说明书

Raltegravir potassium

Print
Chemical Structure| 871038-72-1 同义名 : MK 0518 potassium;Raltegravir (potassium salt);MK-0518
CAS号 : 871038-72-1
货号 : A100140
分子式 : C20H20FKN6O5
纯度 : 98+%
分子量 : 482.507
MDL号 : MFCD12031642
存储条件：

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

液体 -20°C:3-6个月-80°C:12个月
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
动物实验配方：
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].
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 - -
实验方案
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
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