ML133 HCl 1222781-70-5

 ML-133 HCl

分子式：C19H19NO.HCl   分子量：313.82

 

产品描述

ML133是选择性钾离子通道YZ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。

靶点

Kir2.1

         

IC50

290 nM

         

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.

体内研究

 

溶解性

DMSO 63 mg/mL，水 <1 mg/mL，醇 6 mg/mL

稳定性

2年 -20°C粉状，6月-80°C溶于DMSO