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RHC 80267

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Chemical Structure| 83654-05-1 同义名 : U-57908
CAS号 : 83654-05-1
货号 : A1226769
分子式 : C20H34N4O4
纯度 : 99%+
分子量 : 394.508
MDL号 : MFCD00210844
存储条件：

粉末 Sealed in dry,Room Temperature

液体 -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 25 mg/mL(63.37 mM)，配合低频超声助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO
动物实验配方：
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]
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

2.53mL

0.51mL

0.25mL

12.67mL

2.53mL

1.27mL

25.35mL

5.07mL

2.53mL
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