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雷特格韦 (MK-0518)

强大的HIV-1整合酶抑制剂
规格或纯度: ≥97%
有货

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货号 (SKU) 包装规格 是否现货 价格 数量
R129802-5mg 5mg 现货 Stock Image
R129802-10mg 10mg 现货 Stock Image
R129802-50mg 50mg 现货 Stock Image
R129802-250mg 250mg 现货 Stock Image
R129802-1g 1g 现货 Stock Image

基本描述

规格或纯度 ≥97%
英文名称 Raltegravir (MK-0518)
别名 雷特格韦
英文别名 Isentress;N-(2-(4-(4-Fluorobenzylcarbamoyl)-5-hydroxy-1-methyl-6-oxo-1,6-dihydropyrimidin-2-yl)propan-2-yl)-5-methyl-1,3,4-oxadiazole-2-carboxamide; N-((4-Fluorophenyl)methyl)-1,6-dihydro-5-hydroxy-1-methyl-2-(1-methyl-1-(((5-methyl-1,3,4-oxadiazol-2-yl)c
生化机理 Raltegravir is a potent HIV-1 integrase inhibitor. Raltegravir sensitizes S217Q PFV IN to the same extent as the WT enzyme. Raltegravir is potently active against HIV-1 in vitro. Raltegravir is also active against HIV-2 in CEMx174 cells. Raltegravir weakly inhibits hepatic cytochrome P450 activity. Raltegravir effectively attenuates viral replication. Raltegravir efficiently inhibits SIVmac251 replication in acutely infected human lymphoid CD4+ T-cell lines MT-4 and CEMx174.Raltegravir is a potent HIV-1 integrase inhibitor. It inhibits both\xa0wild-type and S217Q PFV integrase with IC 50 of 90 nM and 40 nM in cell-free assays, respectively. It is far less potent against the S217H PFV integrase mutant (IC 50 = 900 nM).
储存温度 -20°C储存
运输条件 超低温冰袋运输
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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.

Raltegravir (MK-0518) is a potent integrase (IN) inhibitor for WT and S217Q PFV IN with IC50 of 90 nM and 40 nM, respectively.
A potent integrase strand transfer inhibitor for (PFV) IN.

名称和标识符

IUPAC Name N-[2-[4-[(4-fluorophenyl)methylcarbamoyl]-5-hydroxy-1-methyl-6-oxopyrimidin-2-yl]propan-2-yl]-5-methyl-1,3,4-oxadiazole-2-carboxamide
INCHI InChI=1S/C20H21FN6O5/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)
InChi Key CZFFBEXEKNGXKS-UHFFFAOYSA-N
Canonical 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
分子式

C20H21FN6O5

PubChem CID 54671008
分子量 444.42

化学和物理性质

溶解性 DMSO 89 mg/mL Water Ethanol

关联配体

Ligand ID 11571
名称 raltegravir
别名 Isentress®
类别 Synthetic organic
学名 4-amino-N-(4,6-dimethylpyrimidin-2-yl)benzenesulfonamide
生物活性评价 Raltegravir (MK-0518) inhibits wild type HIV integrase with an IC50 of 40 nM .
评价 Raltegravir (MK-0518) is an HIV integrase inhibitor (integrase strand transfer inhibitor) .

参考文献

1. Rowley M.  (2008)  The discovery of raltegravir, an integrase inhibitor for the treatment of HIV infection..  Prog Med Chem,  46  (13):  (1-28).  [PMID:18381123]

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