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Raltegravir sodium
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
CAS NO:1292804-07-9
包装与价格:
包装价格(元)
5 mg电议
50 mg电议
100 mg电议

产品介绍
Raltegravir (MK 0518) sodium 是一种有效的、具有口服活性的 HIV 整合酶(IN)抑制剂。

产品描述

Raltegravir (MK 0518) sodium is a potent and orally active integrase (IN) inhibitor, used to treat HIV infection.

体外活性

PFV IN carrying the S217H substitution is 10-fold less susceptible to Raltegravir with IC 50 of 900 nM. PFV IN displays 10% of WT activity and is inhibited by Raltegravir with an IC 50 of 200 nM, indicating a appr twofold decrease in susceptibility to the IN strand transfer inhibitor (INSTI) compared with WT IN. S217Q PFV IN is as sensitive to Raltegravir as the WT enzyme [1]. Raltegravir is metabolized by glucuronidation, not hepatically. 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 IC 95 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 [2]. Raltegravir cellular permeativity is reduced in the presence of magnesium and calcium [3]. Raltegravir and related HIV-1 integrase (IN) strand transfer inhibitors (INSTIs efficiently block viral replication [4]. In acutely infected human lymphoid CD4 + T-cell lines MT-4 and CEMx174, SIVmac251 replication is efficiently inhibited by Raltegravir, which shows an EC 90 in the low nanomolar range [5].

体内活性

Raltegravir induces viro-immunological improvement of nonhuman primates with progressing SIVmac251 infection. One non-human primate shows an undetectable viral load following Raltegravir monotherapy [5].

Cas No.

1292804-07-9

分子式

C20H20FN6NaO5

分子量

466.4

储存和溶解度

(< 1 mg/ml refers to the product slightly soluble or insoluble )
Powder: -20°C for 3 years
In solvent: -80°C for 2 years