475741
MAGL Inhibitor III, JZL184
The MAGL Inhibitor III, JZL184, also referenced under CAS 1101854-58-3, controls the biological activity of MAGL.
别名:
MAGL Inhibitor III, JZL184, 4-Nitrophenyl-4-(dibenzo[d][1,3]dioxol-5-yl(hydroxy)methyl)piperidine-1-carboxylate, Monoacylglycerol Lipase Inhibitor III, JZL184
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About This Item
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质量水平
方案
≥97% (HPLC)
表单
solid
制造商/商品名称
Calbiochem®
储存条件
OK to freeze
protect from light
颜色
white to off-white
溶解性
DMSO: 50 mg/mL
运输
wet ice
储存温度
−20°C
SMILES字符串
[N+](=O)([O-])c1ccc(cc1)OC(=O)N2CCC(CC2)C(O)(c5cc6c(cc5)OCO6)c3cc4c(cc3)OCO4
InChI
1S/C27H24N2O9/c30-26(38-21-5-3-20(4-6-21)29(32)33)28-11-9-17(10-12-28)27(31,18-1-7-22-24(13-18)36-15-34-22)19-2-8-23-25(14-19)37-16-35-23/h1-8,13-14,17,31H,9-12,15-16H2
InChI key
SEGYOKHGGFKMCX-UHFFFAOYSA-N
一般描述
A cell-permeable, blood-brain-barrier-permeant, and orally available carbamate compound that selectively inhibit MAGL (monoacylglycerol lipase) activity over FAAH (fatty acid amide hydrolase) and 35 other murine brain serine hydrolases, both in vitro (IC50 = 6 - 8 nM against 2-AG hydrolysis by MAGL vs. 4 µM against anandamide/AEA hydrolysis by FAAH) and in mice in vivo (5-fold 2-AG enhancement and 75% MAGL activity inhibition in brain membrane from mice 4 hr after a single JZL184 dosage at 4 mg/kg via i.p.) in an irreversible, time- and dose-dependent manner. A great complement to the FAAH inhibitor URB597 (Cat. No. 341249) in differentiating the roles of CB1 and CB2 (type I and II cannabinoid receptors) in eCB- (endocannabinoid) mediated cellular signaling and in vivo physiological effects. Reported to be equally effective against human and murine MAGL, but inhibit rat MAGL with a ~10-fold lower potency.
A cell-permeable, blood-brain-barrier-permeant, and orally available carbamate compound that selectively inhibit MAGL (monoacylglycerol lipase) activity over FAAH (fatty acid amide hydrolase) and 35 other murine brain serine hydrolases, both in vitro (IC50 = 6-8 nM against 2-AG hydrolysis by MAGL vs. 4 µM against anandamide/AEA hydrolysis by FAAH) and in mice in vivo (5-fold 2-AG enhancement and 75% MAGL activity inhibition in brain membrane from mice 4 hr after a single JZL184 dosage at 4 mg/kg via i.p.) in an irreversible, time- and dose-dependent manner. A great complement to the FAAH inhibitor URB597 (Cat. No. 341249) in differentiating the roles of CB1 and CB2 (type I and II cannabinoid receptors) in eCB- (endocannabinoid) mediated cellular signaling and in vivo physiological effects. Reported to be equally effective against human and murine MAGL, but inhibit rat MAGL with a ~10-fold lower potency.
警告
Toxicity: Standard Handling (A)
重悬
Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.
其他说明
Nomura, D.K., et al. 2010. Cell140, 49.
Long, J.Z., et al. Nature Chem. Biol.16, 744.
Long, J.Z., et al. 2009. Nature Chem. Biol.5, 37.
Pan, B., et al. 2009. J. Pharmacol. Exp. Ther.331, 591.
Long, J.Z., et al. Nature Chem. Biol.16, 744.
Long, J.Z., et al. 2009. Nature Chem. Biol.5, 37.
Pan, B., et al. 2009. J. Pharmacol. Exp. Ther.331, 591.
法律信息
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
储存分类代码
11 - Combustible Solids
WGK
WGK 2
闪点(°F)
Not applicable
闪点(°C)
Not applicable
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