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MK-2048,IN和INR263K抑制剂

MK-2048 （订货以英文为准）

编号：M127457
CAS号：869901-69-9
分子式：C21H21CLFN5O4
分子量：461.87
货号 品牌 包装 目录价 您的价格 库存 数量 购买
M127457-5mg 阿拉丁 5mg ¥1274.90
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M127457-50mg 阿拉丁 50mg ¥6247.90
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M127457-10mg 阿拉丁 10mg ¥1784.90
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M127457-1mg 阿拉丁 1mg ¥786.90
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产品名称 MK-2048
中文名称 MK-2048,IN和INR263K抑制剂
CAS号 869901-69-9
分子式（M.F.） C21H21CLFN5O4
分子量（M.W.） 461.87
储存条件 -20°C储存
溶解性DMSO 9 mg/mL Water <1 mg/mL Ethanol <1 mg/mL
存贮条件储存温度-20°C
备注MK-2048 is a potent inhibitor of integrase (IN) and INR263K with IC50 of 2.6 nM and 1.5 nM, respectively.
生化机理MK-2048 is a second generation integrase inhibitor, intended to be used against HIV infection. MK-2048 inhibits subtype B and subtype C integrase activities. MK-2048 inhibits R263K mutants slightly more effectively than G118R mutants. MK-2048 inhibits S217H intasome and, by contrast, MK-2048 remains fully active against the N224H intasome. MK-2048 displays substantially lower dissociation rates compared with raltegravir, another integrase inhibitor. MK-2048 is active against viruses resistant to RAL and EVG. MK-2048 exposure leads to the selection of G118R as a possible novel resistance mutation after 19 weeks. MK-2048, with continued pressure, subsequently leads to an additional substitution, at position E138K, after 29 weeks, within the IN gene. Although the G118R mutation alone confers only slight resistance to MK-2048 but not to RAL or EVG, its presence arouses a dramatic reduction in viral replication capacity compared to wild-type NL4-3. E138K both partially restores viral replication capacity and also contributes to increased levels of resistance against MK-2048.
别名Pyrazino[1',2':1,5]pyrrolo[2,3-d]pyridazine-4-carboxamide, 2-[(3-chloro-4-fluorophenyl)methyl]-8-ethyl-1,2,6,7,8,9-hexahydro-10-hydroxy-N,6-dimethyl-1,9-dioxo-, (6S)-;Pyrazino[1',2':1,5]pyrrolo[2,3-d]pyridazine-4-carboxamide, 2-[(3-chloro-4-fluorophenyl)methyl]-8-ethyl-1,2,6,7,8,9-hexahydro-10-hydroxy-N,6-dimethyl-1,9-dioxo-, (6S)-
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