(4-甲氧基苄基)(1-萘基甲基)胺盐酸盐
发布者：信康 浏览次数：
产品名称:(4-甲氧基苄基)(1-萘基甲基)胺盐酸盐CAS:1222781-70-5别名：(4-甲氧基苄基)(1-萘基甲基)胺盐酸盐;N-[(4-甲氧基苯基)甲基]-1-萘甲胺盐酸盐;ML133HCL(4-甲氧基苄基)(1-萘基甲基)胺盐酸盐;N-[(4-METHOXYPHENYL)METHYL]-1-NAPHTHALENEMETHANAMINEHYDROCHLORIDE英文名：ML 133 Hydrochloride
[] - 生物活性ML133 HCl是一种选择性钾离子通道抑制剂，作用于Kir2.1， IC50为1.8 μM (pH 7.4)和290 nM (pH 8.5)，对Kir1.1没有作用效果，对Kir4.1和Kir7.1具有微弱的作用活性。
- 体外研究The ratio of total concentration of extracellular ML133 versus intracellular ML133 is 1:0.13 at pH 6.5, 1:9.09 at pH 8.5. ML133 is clean against 3A4 and 2C9 (IC50 >30 μM), displays moderate inhibition of 1A2 (IC50 = 3.3 μM) but proves to be a potent inhibitor of 2D6 (IC50 = 0.13 μM) in CYP450 assay. ML133 is highly protein bound (>99%) in both human and rat and also displays high intrinsic clearance in both species. ML133 (10 μM) is not displaced by K+ influx from the wild-type Kir2.1 in HEK 293 cells. M1 and/or M2 transmembrane domains contain the critical molecular determinant for ML133 inhibition of Kir2.1, especially D172 and I176.
