MCE 的所有产品仅用作科学研究或药证申报，我们不为任何个人用途提供产品和服务。

URB602

CAS No. : 565460-15-3

MCE 站：URB602

产品活性：URB602 是一种选择性的单酰基甘油脂肪酶 (MGL) 抑制剂，非竞争性抑制大鼠脑 MGL，IC₅₀ 为 28±4 μM。

研究领域：Others

作用靶点：Others

In Vitro: Without URB602, the apparent Michaelis constant (K_m) of MGL for 2-AG is 24±1.7 μM and the maximum velocity (V_max) is 1814±51 nmol min per mg protein; with URB602, the K_m is 20±0.4 μM and the V_max 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.

In Vivo: 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.

相关产品：Bioactive Compound Library Plus  |  Anti-Cancer Compound Library  |  PEG300  |  SBE-β-CD  |  Corn oil  |  Tween 80  |  Polyethylene glycol 12-hydroxystearate  |  JC-1  |  Lipopolysaccharides  |  DTT  |  (2-Hydroxypropyl)-β-cyclodextrin  |  Methyl-β-cyclodextrin  |  CFSE  |  Digitonin  |  D-Luciferin potassium salt  |  Thiazolyl Blue  |  Biotin  |  3X FLAG peptide TFA  |  Monocrotaline  |  Nile Red  |  Auxinole  |  Tocofersolan  |  FLAG peptide  |  IPTG  |  Yoda 1  |  Cremophor EL  |  GsMTx4 TFA  |  Propidium Iodide  |  DAPI dihydrochloride  |  Calcein-AM  |  Sodium carboxymethyl cellulose (Viscosity:800-1200 mPa.s)

品牌介绍:
•   MCE (MedChemExpress) 拥有数百种全球独家化合物，我们致力于为全球科研客户提供*新*全的高品质小分子活性化合物；
•   10,000 多种高选择性抑制剂、激动剂涉及各热门信号通路及疾病领域；
•   设有专业的实验中心和严格的质控、验证体系；
•   提供 LC/MS、NMR、HPLC、手性分析、元素分析等各项质检报告，确保产品的高纯度、高品质；
•   产品的生物活性多经各国客户实验验证；
•   Nature, Cell, Science 等多种期刊及制药收录了MCE客户的科研成果；
•   专业团队跟踪*新的制药及生命科学研究进展，为您提供全球*新的活性化合物；
•   与世界各大制药公司及知名科研机构建立了长期的合作。