LY2183240 是大麻素摄取阻滞剂。它是内源性大麻素降解酶脂肪酸酰胺水解酶的有效共价抑制剂。它抑制脂肪酸酰胺水解酶 (FAAH) 活性,IC50 为12.4 nM。它也抑制其他几种脑丝氨酸水解酶,对 MAG 脂肪酶、bh6 和 KIAA1363 的 IC50分别为 5.3、0.09 和 8.2 nM。
产品描述
LY2183240 inhibits fatty acid amide hydrolase (FAAH) activity (IC50 = 12.4 nM). LY2183240 is a novel and highly effective blocker of anandamide uptake (IC50 = 270 pM).
体外活性
LY2183240 increases brain anandamide concentration and exerts antinociceptive effects in the formalin model of pain, anandamide uptake Following i.p. administration in rats.
Cas No.
874902-19-9
分子式
C17H17N5O
分子量
307.35
储存和溶解度
DMSO:50 mg/mL (162.68 mM),Need ultrasonic
Powder: -20°C for 3 years
In solvent: -80°C for 2 years