URB602

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

URB602是一种特异性单酰基甘油脂肪酶（MGL）抑制剂，通过非竞争性机制抑制大鼠脑MGL（IC50：28±4 μM）。

URB602 is a selective inhibitor of monoglycerol lipase (MGL), exhibiting an IC50 of 28 μM for the rat brain enzyme. Pretreatment with the monoacylglycerol lipase inhibitor URB602 protects from the long-term consequences of neonatal hypoxic-ischemic brain injury in rats. URB602 inhibits monoacylglycerol lipase and selectively blocks 2-arachidonoylglycerol degradation in intact brain slices.

Without URB602, the apparent Michaelis constant (Km) of MGL for 2-AG is 24±1.7 μM and the maximum velocity (Vmax) is 1814±51 nmol min per mg protein; with URB602, the Km is 20±0.4 μM and the Vmax is 541±20 nmol min per mg protein (n=4). When organotypic slice cultures of rat forebrain are incubated with URB602 (100 μM), both baseline and Ca2+-ionophore-stimulated 2-arachidonoylglycerol (2-AG) concentrations are increased. URB602 is an inhibitor of monoacylglycerol lipase (MGL), a serine hydrolase involved in the biological deactivation of the endocannabinoid 2-arachidonoyl-sn-glycerol (2-AG). URB602 weakly inhibits recombinant MGL (IC50=223±63 μM) through a rapid and noncompetitive mechanism.

URB602 at doses of 20 and 40 mg/kg tends to reduce upper GI transit and slow colonic propulsion. When taken together as whole gut transit, URB602 dose dependently inhibits transit (P<0.05) compared with the vehicle control group. The inhibitory action of 40 mg/kg URB602 on whole gut transit is absent in these mice, indicating CB1 receptor involvement in the inhibitory action. URB602 decreases the AUC of pain behaviour during the early phase of the formalin test with an ED50 of 0.06±0.028 μg for JZL184 and 120±51.3 μg for URB602 in adult male Sprague-Dawley rats. Both MGL inhibitors also suppresses pain behaviour during the late phase of formalin pain, with an ED50 of 0.03±0.011 μg for JZL184 and 66±23.9 μg for URB602.

URB602, URB-602, URB 602

Others

Other Targets

rat brain MGL

Cancer

——

565460-15-3

295.38

C19H21NO2

>98% (HPLC)

DMSO : ≥ 31 mg/mL; 104.95 mM

C1CCC(CC1)OC(=O)Nc1cccc(c1)c1ccccc1

cyclohexyl [1,1'-biphenyl]-3-ylcarbamate

(-20℃)

With Ice Pack

≥ 2 years