RHC 80267
(Synonyms: 1,6-双(环己基脒基羰基氨基)己烷,U-57908) 目录号 : GC12411
An inhibitor of DAGL
Cas No.:83654-05-1
Sample solution is provided at 25 µL, 10mM.
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Quality Control & SDS
- View current batch:
- Purity: >99.50%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
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.
| Cas No. | 83654-05-1 | SDF | |
| 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 SMILES | O/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°C |
| General tips | 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。 储备液的保存方式和期限：-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 2.5348 mL | 12.6739 mL | 25.3479 mL |
| 5 mM | 0.507 mL | 2.5348 mL | 5.0696 mL |
| 10 mM | 0.2535 mL | 1.2674 mL | 2.5348 mL |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
3. 以上所有助溶剂都可在 GlpBio 网站选购。