| 货号 (SKU) | 包装规格 | 是否现货 | 价格 | 数量 |
|---|---|---|---|---|
| R407876-1ml |
1ml |
现货  |
|
| 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。 |
| 储存温度 | -80℃储存 |
| 运输条件 | 超低温冰袋运输 |
| 产品介绍 |
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 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 lines： Concentrations：0.0001-1 μM Incubation Time：5 days Powder Purity:≥97% |
| 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 | 54671008 |
| 分子量 | 444.42 |
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