83654-05-1|Cyclohexanone O-((6-((((cyclohexylideneamino)oxy)carbonyl)amino)hexyl)carbamoyl) oxime|CsnPharm

CAS No.: 83654-05-1

RHC 80267 Catalog No. CSN25327

Synonyms: U-57908

RHC 80267 is a diacylglycerol (DAG) lipase inhibitor and an important second messenger in signal transduction pathways.

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靶点选择性

生物活性

实验方案

技术信息

生物活性

描述RHC-80267 is a potent and selective diacylglycerol lipase inhibitor with an IC50 value of 4µM for canine platelet diglyceride lipase.^[1] In the circular smooth muscle isolated from the stomach antrum of guinea pig, RHC-80267 at a concentration of 0.3μM increased the slow potentials from 1.12±0.31 min–1 to 2.43±0.67 min^–1. The refractory period for the generation of slow potentials in smooth muscle cells was also reduced in the presence of 0.3μM RHC-80267.^[2] In rat brain homogenates, RHC-80267 inhibited cholinesterase activity in a concentration-dependent manner with a pIC50 value of 5.39±0.06 (IC50 = 4μM). Pre-incubation of rat artery rings with RHC-80267 (10^-7–10^-5M) resulted in a concentration-dependent leftward shift of the concentration-effect curve to acetylcholine. Pre-incubation with calphostin C (1μM) and RHC-80267 (10μM) decreased the contraction evoked by noradrenaline by 50±9%. In KCl-contracted arteries, pre-incubation with 10μM RHC-80267 led to a leftward shift of the relaxation evoked by acetylcholine.^[3]
作用机制RHC-80267 is a diacylglycerol lipase inhibitor that enhances the activity of protein kinase C by elevating the level of diacylglycerol.^[2]
参考文献

[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 Dec 10;257(23):14006-10
[2] Suzuki H, Kito Y, Fukuta H, Yamamoto Y. 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 Dec;38(6):153-64. doi: 10.1540/jsmr.38.153
[3] Ghisdal P, Vandenberg G, Hamaide MC, Wibo M, Morel N. The diacylglycerol lipase inhibitor RHC-80267 potentiates the relaxation to acetylcholine in rat mesenteric artery by anti-cholinesterase action. Eur J Pharmacol. 2005 Jul 4;517(1-2):97-102. doi: 10.1016/j.ejphar.2005.05.036

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 2.5348 mL
- 12.6740 mL
- 25.3480 mL
- 5 mM
- 0.5070 mL
- 2.5348 mL
- 5.0696 mL
- 10 mM
- 0.2535 mL
- 1.2674 mL
- 2.5348 mL

技术信息

CAS号

83654-05-1

储存条件

粉末: Sealed in dry,Room Temperature

液体: -20°C:3-6 月 -80°C:12月

分子式

C20H34N4O4

运输

蓝冰

分子量

394.51

别名

U-57908

溶解度

DMSO	79.0 mg/mL (200.2 mM)
Water	Insoluble
Ethanol	79.0 mg/mL (200.2 mM)

动物实验配方

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