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RHC 80267
本产品不向个人销售，仅用作科学研究，不用于任何人体实验及非科研性质的动物实验。
RHC 80267图片
CAS NO:83654-05-1
包装与价格：
包装价格(元)
10mg电议
25mg电议
50mg电议
100mg电议

产品介绍
RHC 80267 (U-57908) 是一种有效的选择性二酰基甘油脂肪酶 (DAGL) 抑制剂（在犬血小板中的 IC50 为 4 μM）。
Cas No.83654-05-1
别名1,6-双(环己基脒基羰基氨基)己烷,U-57908
化学名cyclohexanone O-((E)-((6-((E)-(((cyclohexylideneamino)oxy)(hydroxy)methylene)amino)hexyl)imino)(hydroxy)methyl) oxime
Canonical SMILESO/C(O/N=C1CCCCC/1)=N\CCCCCC/N=C(O/N=C2CCCCC/2)\O
分子式C20H34N4O4
分子量394.51
溶解度DMF: 15 mg/ml,DMF:PBS(pH 7.2)(1:1): 0.5 mg/ml,DMSO: 5 mg/ml,Ethanol: 5 mg/ml
储存条件Store at -20℃
General tipsFor obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.
Shipping ConditionEvaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request
产品描述

RHC 80267 is a potent and selective inhibitor of diacylglycerol lipase [1].

Diacylglycerol lipase is a key enzyme in the biosynthesis of the endocannabinoid 2-arachidonoylglycerol and catalyzes the hydrolysis of diacylglycerol.

RHC 80267 is a potent and selective diacylglycerol lipase inhibitor. RHC 80267 inhibited canine platelet diglyceride lipase with IC50 value of 4 μM. RHC 80267 inhibited diacylglycerol lipase released from rat and dog platelets. Also, RHC 80267 induced diglyceride accumulation and inhibited fatty acid accumulation [1]. In smooth muscle isolated from the guinea-pig gastric antrum, RHC-80267 (0.3-1 μM) increased slow potential frequency and reduced the refractory period for slow potentials generation evoked by depolarizing stimuli from 8 s to 5 s. Also, RHC-80267 enhanced the frequency of slow potentials increased by acetylcholine (ACh). RHC 80267 increased diacylglycerol accumulation, which then activated PKC. PKC was involved in regulating the frequency of slow potentials [2]. In rat mesenteric artery contracted with either KCl or noradrenaline, RHC-80267 (0.1-10 μM) enhanced acetylcholine-evoked relaxation. In brain homogenate, RHC-80267 inhibited cholinesterase activity with IC50 value of 4 μM in a concentration-dependent way. These results suggested that the enhancement of acetylcholine-evoked responses by RHC-80267 was caused by the inhibition of the cholinesterase activity [3].

References:
[1].  Sutherland CA, Amin D. Relative activities of rat and dog platelet phospholipase A2 and diglyceride lipase. Selective inhibition of diglyceride lipase by RHC 80267. J Biol Chem, 1982, 257(23): 14006-14010.
[2].  Suzuki H, Kito Y, Fukuta H, et al. Effects of RHC-80267, an inhibitor of diacylglycerol lipase, on excitation of circular smooth muscle of the guinea-pig gastric antrum. J Smooth Muscle Res, 2002, 38(6): 153-164.
[3].  Ghisdal P, Vandenberg G, Hamaide MC, et al. The diacylglycerol lipase inhibitor RHC-80267 potentiates the relaxation to acetylcholine in rat mesenteric artery by anti-cholinesterase action. Eur J Pharmacol, 2005, 517(1-2): 97-102.