DH376 is a highly potent , in vivo active compound that inhibits DAGLα in a time- and dose dependent manner in mouse brain. DH376 showed picomolar activity
Uses
DH-376 is a potent diacylglycerol lipase inhibitor with pIC50 values of 8.6 and 8.9 for ABHD6 and DAGLα, respectively. DH-376 prevents fasting-induced refeeding of mice[1]. DH-376 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
in vivo
DH-376 (50 mg/kg; i.p.) reduces fasting-induced refeeding of mice[1].
Animal Model:
male C57Bl/6J mice[1]
Dosage:
50 mg/kg
Administration:
intraperitoneal injection
Result:
Inhibitd fasting-induced refeeding.
References
[1] Deng H, et, al. Triazole Ureas Act as Diacylglycerol Lipase Inhibitors and Prevent Fasting-Induced Refeeding. J Med Chem. 2017 Jan 12;60(1):428-440. DOI:10.1021/acs.jmedchem.6b01482