货号 | 3836/50 |
别名 | 4-[Bis(1,3-benzodioxol-5-yl)hydroxy |
供应商 | Tocris |
生物活性 | Potent and selective MAGL inhibitor. Blocks hydrolysis of the endocannabinoid 2-arachidonyl glycerol (2-AG) in vivo in the mouse brain (IC50 = 8 nM). Potentiates depolarization-induced suppression of excitability in cerebellar Purkinje neurons. Exhibits >300-fold selectivity for MAGL over FAAH in vitro. Attenuates nociception in neuropathic and inflammatory pain models. Also reduces free fatty acid levels in primary tumors. |
运输条件 | Blue Ice |
存放说明 | -20℃ |
纯度 | >98 % |
计算分子量 | 520.49 |
分子式 | C27H24N2O9 |
可溶性/溶解性 | Soluble to 100 mM in DMSO |
参考文献 | Kinseyet al (2013) Repeated low-dose administration of the monoacylglycerol lipase inhibitor JZL184 retains cannabinoid receptor type 1-mediated antinociceptive and gastroprotective effects. J.Pharmacol.Exp.Ther. 345 492. PMID: 23412396. Zhanget al (2012) Dysregulated lipid metabolism in cancer. World J.Biol.Chem. 3 167. PMID: 22937213. Longet al (2009) Selective blockade of 2-arachidonylglycerol hydrolysis produces cannabinoid behavioral effects. Nat.Chem.Biol. 5 37. PMID: 19029917. Panet al (2009) Blockade of 2-arachidonylglycerol hydrolysis by selective monoacylglycerol lipase inhibitor 4-nitrophenyl 4-(dibenzo[d][1,3]dioxol-5-yl(hydroxy)methyl)piperidine-1-carboxylate (JZL184) enhances retrograde endocannabinoid signaling. J.Pharm.Exp.Ther. 331 591. PMID: 19666749. |