诚信认证:
工商注册信息已核实!
MK-2048
品牌 | 厂商性质 | 产地 | 货期 |
---|---|---|---|
阿拉丁 | 生产商 | 上海 | 现货 |
货号 | CAS号 | 操作 |
---|---|---|
M127457-10mg | 869901-69-9 | 询底价 |
M127457-1mg | 869901-69-9 | 询底价 |
M127457-50mg | 869901-69-9 | 询底价 |
M127457-5mg | 869901-69-9 | 询底价 |
- 分子式 C21H21ClFN5O4
- 分子量461.87
属性
溶解性 |
|
存贮条件 | 储存温度-20°C |
描述
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)- |
MK-2048信息由上海阿拉丁生化科技股份有限公司为您提供,如您想了解更多关于MK-2048报价、型号、参数等信息,欢迎来电或留言咨询。
注:该产品未在中华人民共和国食品药品监督管理部门申请医疗器械注册和备案,不可用于临床诊断或治疗等相关用途