首页 工具
登录
购物车
URB602

URB602

产品编号 T3591   CAS 565460-15-3

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。

TargetMol的所有产品和服务仅用于科学研究,不能被用于人体,我们也不向个人提供产品和服务。
URB602 Chemical Structure
URB602, CAS 565460-15-3
规格 价格/CNY 货期 数量
5 mg ¥ 225 现货
10 mg ¥ 398 现货
25 mg ¥ 657 现货
50 mg ¥ 1,160 现货
100 mg ¥ 1,980 现货
500 mg ¥ 4,900 现货
1 mL * 10 mM (in DMSO) ¥ 251 现货
产品目录号及名称: URB602 (T3591)
点击图片重新获取验证码
选择批次  
纯度: 99.81%
纯度: 99.64%
更多批次查询请联系客服
生物活性
化学信息
存储 & 溶解度
参考文献
产品描述 URB602 is a specific monoacylglycerol lipase (MGL) inhibitor, which inhibits rat brain MGL (IC50: 28±4 μM) through a noncompetitive mechanism.
靶点活性 MGL:28±4 μM
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).
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].
分子量 295.38
分子式 C19H21NO2
CAS No. 565460-15-3

存储

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

溶解度

DMSO: 31 mg/mL

计算器

摩尔浓度计算器
稀释计算器
配液计算器
分子量计算器
=
X
X
X
=
X
=
/
g/mol

输入分子式,点击计算,可计算出产品的分子量。

参考文献

1. Hohmann AG, et al. An endocannabinoid mechanism for stress-induced analgesia. Nature. 2005 Jun 23;435(7045):1108-12. 2. King AR, et al. URB602 inhibits monoacylglycerol lipase and selectively blocks 2-arachidonoylglycerol degradation in intact brain slices. Chem Biol. 2007 Dec;14(12):1357-65. 3. Duncan M, et al. Distribution and function of monoacylglycerol lipase in the gastrointestinal tract. Am J Physiol Gastrointest Liver Physiol. 2008 Dec;295(6):G1255-65. 4. Guindon J, et al. Peripheral antinociceptive effects of inhibitors of monoacylglycerol lipase in a rat model of inflammatory pain. Br J Pharmacol. 2011 Aug;163(7):1464-78.
MJN110 KML29 Atglistatin Y-320 Endothelial lipase inhibitor-1 PF-06795071 WWL70 JJKK 048

相关化合物库

该产品包含在如下化合物库中:
抗肥胖化合物库 代谢化合物库 NO PAINS 化合物库 抗感染化合物库 抑制剂库 经典已知活性库 已知活性化合物库 抗菌活性库 抗代谢疾病化合物库 活性脂质化合物库

剂量换算

对于不同动物的给药剂量换算,您也可以参考 更多...

体内实验配液计算器

请在以下方框中输入您的动物实验信息后点击计算,可以得到母液配置方法和体内配方的制备方法: 比如您的给药剂量是10 mg/kg,每只动物体重20 g,给药体积100 μL,一共给药动物10 只,您使用的配方为5% DMSO+30% PEG300+5% Tween 80+60% ddH2O。那么您的工作液浓度为2 mg/mL。

母液配置方法:2 mg 药物溶于 50 μL DMSO (母液浓度为 40 mg/mL), 如您需要配置的浓度超过该产品的溶解度,请先与我们联系。

体内配方的制备方法:取 50 μL DMSO 主液,加入 300 μL PEG300, 混匀澄清,再加 50 μL Tween 80,混匀澄清,再加 600 μL ddH2O, 混匀澄清。

第一步:请输入动物实验的基本信息
剂量
mg/kg
每只动物体重
g
给药体积
μL
动物数量
第二步:请输入动物体内配方组成,不同的产品配方组成不同,如有配方需求,可先联系我们提供正确的体内配方。
% DMSO
%
% Tween 80
% ddH2O
计算 重置

技术支持

您可能有的问题的答案可以在抑制剂处理说明中找到,包括如何准备库存溶液,如何存储产品,以及基于细胞的分析和动物实验需要特别注意的问题。

Keywords

URB602 565460-15-3 Metabolism Microbiology/Virology Lipase Antibacterial URB 602 Bacterial URB-602 inhibit Inhibitor inhibitor

 

陶术
生物
TargetMol®中国区唯一合作伙伴
点击进入陶术生物官网陶术生物
联系我们
400-820-0310

上海市静安区江场三路238号8楼