雷特格韦钾盐

Raltegravir potassium
871038-72-1

询价 10g 起订

100g 起订

500g 起订

湖北更新日期：2024-07-17

湖北凯隆生物科技有限公司

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产品详情:

中文名称：: 雷特格韦钾盐

英文名称：: Raltegravir potassium

CAS号：: 871038-72-1

品牌：: 湖北凯隆

产地：: 国产

保存条件：: 常温密封干燥储存

纯度规格：: 98HPLC

产品类别：: 原料药

性状：: 白色粉末

含量：: ≥98%

中文名	雷特格韦钾盐
英文名	Raltegravir potassium
别名	拉替拉韦钾雷特格韦钾拉替拉韦钾盐雷特格韦钾盐拉替拉韦钾中间体雷特格韦-13C-D3 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)
英文别名	CS-1293 MK 0518 CS-1950 MK 0518 MK0518 POTASSIUM SALT Raltegravir potassium MK 0518 POTASSIUM SALT MK 0518 potassium salt MK-0518 POTASSIUM SALT ISENTRESS POTASSIUM SALT Isentress potassium salt Raltegravir Potassium Salt 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 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
CAS	871038-72-1
EINECS	682-461-3
化学式	C20H20FN6O5.K
分子量	482.511
InChI	InChI=1/C20H21FN6O5.K/c1-10-25-26-17(32-10)16(30)24-20(2,3)19-23-13(14(28)18(31)27(19)4)15(29)22-9-11-5-7-12(21)8-6-11;/h5-8,28H,9H2,1-4H3,(H,22,29)(H,24,30);/q;+1/p-1
熔点	155-157°C
溶解度	DMSO (微溶，加热)，甲醇 (微溶，加热)，水 (微溶)
存储条件	-20°C Freezer
外观	固体
颜色	White to Light Beige
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.
海关编号	2934990002

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