| RHC 80267diacylglycerol lipase inhibitor |
Sample solution is provided at 25 µL, 10mM.
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Science.2016 Aug 5;353(6299)594-8Nat Nanotechnol.2017 Dec;12(12):1190-1198.Nature Biotechnology.2017 Jun;35(6):569-576Nat Med.2018 Sep 17.Cell.2018 Dec 21. pii: S0092-8674(18)31561-7.Cell.Available online 25 October 2018.Cell.2018 Sep 27. pii: S0092-8674(18)31183-8.Cell.2018 Jun 28;174(1):172-186.e21.Cell.2018 Feb 22;172(5):1007-1021.e17.Cell.2017 Nov 30;171(6):1284-1300.e21.Cell.2017 Aug 17. pii: S0092-8674(17)30869-3.Cell.2017 Jul 13;170(2):312-323Nat Med.2018 Jan 29.Nat Med.2017 Nov;23(11):1342-1351.Cell.2017 Apr 6;169(2):286-300.Cell.2015 Aug 27;162(5):987-1002.Cell.2015 Feb 12;160(4):729-44.Nature Medicine.2017 Apr;23(4):493-500.Cancer Cell.2018 May 14;33(5):905-921.e5.Cancer Cell.2018 Apr 9;33(4):752-769.e8.Cancer Cell.2018 Mar 12;33(3):401-416.e8.Cancer Cell.2017 Aug 14;32(2):253-267.e5.Nat Methods.2018 Jul;15(7):523-526.Cell Stem Cell.2018 May 3;22(5):769-778.e4.Cell Stem Cell.2017 Nov 20. pii: S1934-5909(17)30375-2.Quality Control & MSDS
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| Cas No. | 83654-05-1 | SDF | Download SDF |
| Synonyms | N/A | ||
| Chemical Name | cyclohexanone O-((E)-((6-((E)-(((cyclohexylideneamino)oxy)(hydroxy)methylene)amino)hexyl)imino)(hydroxy)methyl) oxime | ||
| Canonical SMILES | O/C(O/N=C1CCCCC/1)=NCCCCCC/N=C(O/N=C2CCCCC/2)O | ||
| Formula | C20H34N4O4 | M.Wt | 394.51 |
| Solubility | Soluble in DMSO | Storage | Store at -20°C |
| Physical Appearance | A crystalline solid | Shipping Condition | Evaluation sample solution : ship with blue ice.All other available size:ship with RT , or blue ice upon request |
| General tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months. | ||
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.
