KML29 是一种口服具有活性的、高度选择性的不可逆MAGL抑制剂,其对小鼠、大鼠和人的IC50值分别为15 nM、43 nM 和 5.9 nM。它对FAAH在内的其他中心和外周丝氨酸水解酶的交叉反应极小。
产品描述
KML29 is highly selective and effective monoacylglycerol lipase (MAGL) inhibitor. It has effective inhibition of human/mouse/rat MAGL (IC50: 5.9/15/43 nM). It has not inhibitory for FAAH (IC50 >50 μM). It also effectively and selectively blocks hydrolysis of 2-arachidonoylglycerol (2-AG) in mice (IC50: 2.5 nM, 2-AG; >50 μM, AEA).
体内活性
DprE1-IN-2 has efficacy in a rodent model of tuberculosis.
Cas No.
1380424-42-9
分子式
C24H21F6NO7
分子量
549.42
储存和溶解度
DMSO:10 mM
Powder: -20°C for 3 years
In solvent: -80°C for 2 years