计算溶液所需的质量、体积或浓度。
| 活性类型 | 活性值-log(M) | 作用机制 | 期刊 | 参考文献(PubMed IDs) |
|---|
有货
为什么选择此级别
Moligand™ 级 ，适用于对基线干扰要求严格的色谱和分析工作流程。
储存与运输
-80℃储存。特低温运输 。请查阅批次 COA 获取详细规格。
质量文档
SDS、COA、产品数据表及规格说明书均可下载。可通过批号查询获取批次 COA。
文献证明
在色谱分析、有机合成和交叉偶联反应领域已被 1 篇同行评审文献引用。
概述
Raltegravir (MK-0518)是一种有效的整合酶链转移抑制剂，作用于WT和S217Q原型泡沫病毒(PFV)整合酶，IC50分别为90 nM和40 nM。A potent integrase strand transfer inhibitor for (PFV) IN.
Information
Raltegravir (MK-0518) Raltegravir (MK-0518) is a potent integrase (IN) inhibitor for WT and S217Q PFV IN with IC50 of 90 nM and 40 nM in cell-free assays, respectively. It shows greater than 1000-fold selectivity for HIV-1 IN over several related Mg2+-d
In vitro
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.
In vivo
Raltegravir induces viro-immunological improvement of nonhuman primates with progressing SIVmac251 infection. One non-human primate shows an undetectable viral load following Raltegravir monotherapy.
Cell Data
cell lines：
Concentrations：0.0001-1 μM
Incubation Time：5 days
Powder Purity:≥97%
规格
别名
雷替拉韦 (MK-0518)
英文别名
N-(4-fluorobenzyl)-5-hydroxy-1-methyl-2-(2-(2-methyl-1,3,4-oxadiazole-5-carboxamido)propan-2-yl)-6-oxo-1,6-dihydropyrimidine-4-carboxamide
规格或纯度
Moligand™, 10mM in DMSO
英文名称
Raltegravir (MK-0518)
生化机理
Raltegravir (MK-0518) 是一种强效的整合酶 (IN) 抑制剂，在无细胞实验中对 WT 和 S217Q PFV IN 的 IC50 分别为 90 nM 和 40 nM。与 HCV 聚合酶、HIV 逆转录酶、HIV RNaseH 和人类 α-、β-、γ- 聚合酶等几种相关的 Mg2+ 依赖性酶相比，它对 HIV-1 IN 的选择性超过 1000 倍。
储存条件
-80℃储存
运输条件
特低温运输
名称和识别符
EC号
610-733-3
分子类型
小分子
Isomeric SMILES
CC1=NN=C(O1)C(=O)NC(C)(C)C2=NC(=C(C(=O)N2C)O)C(=O)NCC3=CC=C(C=C3)F
PubChem CID
分子量
444.42
技术文档
高级数据
关联靶点（人）
CCR1
Tchem
CC 趋化因子受体 1 型(C-C chemokine receptor type 1)
(1 活性数据)
质检证书（CoA,COO,BSE/TSE 和分析图谱)
C of A & Other Certificates(BSE/TSE, COO):
输入批号以搜索分析图谱:
技术文档和文章
此产品的引用文献
溶液计算器
产品仅提供给经过验证的企业、机构和合格的专业人员用于研发。不适用于人类、动物、诊断或治疗。
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