Endocannabinoids such as 2-arachidonoyl glycerol (2-AG; Item No. 62160) and arachidonoyl ethanolamide (AEA; Item No. 90050) are biologically active lipids that are involved in a number of synaptic processes including activation of cannabinoid receptors. Monoacylglycerol lipase (MAGL) is a serine hydrolase responsible for the hydrolysis of 2-AG to arachidonic acid (Item No. 90010) and glycerol, thus terminating its biological function. MJN110 is an N-hydroxysuccinimidyl carbamate that inhibits MAGL (IC50 = 9.1 nM) and to a lesser extent ABHD6 with potent selectivity over FAAH (IC50 > 10 µM) and other brain serine hydrolases.{28778} It can inhibit 2-AG hydrolysis (IC50 = 2.1 nM) with no effect on AEA hydrolysis up to 50 µM.{28778} At 5 mg/kg, MJN110 has been shown to alleviate mechanical allodynia in a rat model of diabetic neuropathy.{28778}
产品描述
An inhibitor of MAGL (IC50 = 9.1 nM) and to a lesser extent ABHD6 with potent selectivity over FAAH (IC50 > 10 µM) and other brain serine hydrolases; inhibits 2-AG hydrolysis (IC50 = 2.1 nM) with no effect on AEA hydrolysis up to 50 µM; alleviates mechanical allodynia in a rat model of diabetic neuropathy at 5 mg/kg
