化合物URB602 T3591

Product Introduction
Bioactivity


英文名: URB602

描述: URB602 是选择性单酰基甘油脂肪酶 (MGL) 抑制剂，非竞争性抑制大鼠脑 MGL，IC50为 28±4 μM。

激酶实验: Samples containing either URB602 (300 μM), MGL (1.4 pM), or both URB602 and MGL are incubated at 37°C for 30 min in assay buffer. At various time points, the reaction is stopped with an equal volume of ice-cold methanol and directly analyzed in positive ionization mode by LC/MS. A SB-CN column (150×2.1 mm i.d., 5 μm) eluted is used with a linear gradient of methanol in water containing 0.25% acetic acid and 5 mM ammonium acetate (from 60% to 100% of methanol in 8 min) at a flow rate of 0.5 mL/min with column temperature at 50°C. Capillary voltage is set at 4 kV and fragmentor voltage is 100V. Nebulizer pressure is set at 60 psi. N2 is used as drying gas at a flow rate of 13 liters/min and a temperature of 350°C. ESI is in the positive mode and a full scan spectrum is acquired from m/z 100 to 600. Extracted ion chromatograms are used to quantify URB602 ([M+H]+, m/z 296)[2].

体外活性: The apparent Km of MGL for 2-AG is 24±1.7 μM and the Vmax is 1814±51 nmol/min/mg protein; with URB602, the Km is 20±0.4 μM and the Vmax is 541±20 nmol/min/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[1]. URB602 weakly inhibits recombinant MGL (IC50: 223±63 μM) through a rapid and noncompetitive mechanism.

体内活性: URB602 (20-40 mg/kg) can reduce upper GI transit and slow colonic propulsion. In whole gut transit, URB602 dose-dependently inhibits transit (P<0.05) compared with the vehicle control group. The inhibitory action of URB602 (40 mg/kg) on whole gut transit is absent in these mice, demonstrating CB1 receptor involvement in the inhibitory action[3]. During the early phase of the formalin test, URB602 decreases the AUC of pain behavior for JZL184 (ED50: 0.06±0.028 μg) and for URB602 (ED50: 120±51.3 μg) in adult male Sprague-Dawley rats. Both MGL inhibitors also suppress pain behavior during the late phase of formalin pain for JZL184 (ED50: 0.03±0.011 μg) and for URB602 (ED50: 66±23.9 μg).

存储条件: Powder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度: DMSO : 31 mg/mL


关键字: URB 602 | Bacterial | URB-602 | inhibit | URB602 | Inhibitor

相关产品: JZP-430 | MAGL-IN-1 | Endothelial lipase inhibitor-1 | XEN445 | JJKK 048 | MAGL-IN-4 | JW 642 | NF-1819 | Beta-Sitosterol | JNJ-42226314

相关库: Bioactive Lipid Compound Library | Bioactive Compounds Library Max | Anti-Metabolism Disease Compound Library | Inhibitor Library | Anti-Obesity Compound Library | Metabolism Compound Library | Anti-Bacterial Compound Library | NO PAINS Compound Library | Bioactive Compound Library | Anti-Infection Compound Library

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注：该产品未在中华人民共和国食品药品监督管理部门申请医疗器械注册和备案，不可用于临床诊断或治疗等相关用途