雷特格韦钾盐
CAS:871038-72-1
英文名称:Raltegravir potassium
分子式:C₂₀H₂₀FKN₆O₅
分子量:482.51 

中文别名: N-(2-(4-(4-氟苄基氨基甲酰基)-5-羟基-1-甲基-6-氧代-1,6-二氢嘧啶-2-基)丙-2-基)-5-甲基-1,3,4-恶二唑-2-甲酰胺钾盐

英文别名:N-[(4-Fluorophenyl)methyl]-1,6-dihydro-5-hydroxy-1-methyl-2-[1-methyl-1-[[(5-methyl-1,3,4-oxadiazol-2-yl)carbonyl]amino]ethyl]-6-oxo-4-pyrimidinecarboxamide potassium salt; MK 0518

CAS NO.871038-72-1

英文品名 Raltegravir potassium

中文品名雷特格韦钾盐

分子式C20H20FKN6O5

分子量444.41

规格/纯度98%

供应能力can supply large quantity in kgs scale

别名 MK-0518;Raltegravir Potassium Salt;Raltegravir

产品简述

 Raltegravir Potassium Salt is a potent human immunodeficiency virus (HIV) integrase inhibitor

详细说明

PFV IN carrying the S217H substitution is 10-fold less susceptible to Raltegravir with IC50 of 900 nM. PFV IN displays 10% of WT activity and is inhibited by Raltegravir with an IC50 of 200 nM, indicating a ~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. Raltegravir is metabolized by glucuronidation, not hepatically. Raltegravir has potent in vitro activity against HIV-1, with a 95% inhibitory concentration of 31?0 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. Raltegravir cellular permeativity is reduced in the presence of magnesium and calcium. Raltegravir and related HIV-1 integrase (IN) strand transfer inhibitors (INSTIs efficiently block viral replication. 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.

雷特格韦
英文名称： Raltegravir
中文名称： 雷特格韦
分子式： C20H21FN6O5
分子量： 444.42
CAS： 518048-05-0