雷特格韦钾盐 CAS#: 871038-72-1

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雷特格韦钾盐

生物活性靶点体外研究体内研究 用途与合成方法 MSDS 雷特格韦钾盐价格(试剂级) 上下游产品信息

中文名称	雷特格韦钾盐
中文同义词	拉替拉韦钾;拉替拉韦钾中间体;雷特格韦钾盐;雷特格韦-13C-D3;拉替拉韦钾盐;雷特格韦钾;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;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(拉替拉韦中间体)
英文名称	Raltegravir potassium
英文同义词	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;Raltegravir Potassium Salt;MK 0518;CS-1950;CS-1293;Isentress potassium salt;ISENTRESS POTASSIUM SALT;MK0518 POTASSIUM SALT;MK-0518 POTASSIUM SALT;MK 0518 POTASSIUM SALT;MK 0518 potassium salt
CAS号	871038-72-1
分子式	C20H20FN6O5.K
分子量	482.511
EINECS号	682-461-3
相关类别	医药原料;医药中间体;抗生素;小分子抑制剂;小分子抑制剂，天然产物;拉替拉韦中间体;化学试剂;API;Inhibitor;Inhibitors;Intermediates & Fine Chemicals;Pharmaceuticals;All Inhibitors
Mol文件	871038-72-1.mol
结构式

雷特格韦钾盐 性质

雷特格韦钾盐 用途与合成方法

生物活性

Raltegravir Potassium是一种具有口服活性的raltegravir钾盐。Raltegravir是HIV-1 integrase抑制剂。

靶点

体外研究

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. 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. 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 EC     ₉₀    in the low nanomolar range.

体内研究

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

安全信息

MSDS信息

雷特格韦钾盐 价格(试剂级)

雷特格韦钾盐 上下游产品信息