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JZL184 Sale

目录号 : GC14390

A potent and selective inhibitor of MAGL

JZL184 Chemical Structure

Cas No.:1101854-58-3

规格 价格 库存 购买数量
10mM (in 1mL DMSO)
¥420.00
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10mg
¥357.00
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50mg
¥1,365.00
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500mg
¥8,190.00
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1g
¥13,104.00
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产品描述

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JZL184 is a potent and selective inhibitor of MAGL [1].

Monoacylglycerol lipase (MAGL) is a membrane-associated member of the serine hydrolase superfamily and hydrolyzes endocannabinoid 2-arachidonoylglycerol (2-AG) and intracellular triglyceride stores.

JZL184 is a potent and selective MAGL inhibitor. In cerebellar Purkinje neurons, JZL184 (40-120 min) prolonged depolarization-induced suppression of excitation (DSE) in a dose-dependent way, which was mediated by CB1 receptor. In hippocampal CA1 pyramidal neurons, JZL184 (100 nM) significantly prolonged depolarization-induced suppression of inhibition (DSI), which was mediated by CB1 receptor activation. In mouse cerebellar slices, JZL184 (100 nM) significantly enhanced 2-AG (10 μM)-induced depression of EPSCs in Purkinje neurons. These results suggested that MAGL is the primary mechanism by which 2-AG is metabolized [1].

In mice, JZL184 inhibited 2-AG hydrolysis with IC50 value of 8 nM and increased brain 2-AG by 8-fold. The JZL184-treated mice exhibited CB1-dependent behaviors including analgesia, hypomotility and hypothermia [2]. In rats, JZL184 (8 mg/kg) exhibited anxiolytic-like effects via inhibition of MGL mediated 2-AG hydrolysis under high levels of environmental aversiveness [3]. In rats, JZL184 produced antinociception with ED50 values of 0.06 and 0.03 μM in the early phase and the late phase of formalin pain, respectively [4].

References:
[1].  Pan B, Wang W, Long JZ, et al. Blockade of 2-arachidonoylglycerol 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 Pharmacol Exp Ther, 2009, 331(2): 591-597.
[2].  Long JZ, Li W, Booker L, et al. Selective blockade of 2-arachidonoylglycerol hydrolysis produces cannabinoid behavioral effects. Nat Chem Biol, 2009, 5(1): 37-44.
[3].  Sciolino NR, Zhou W, Hohmann AG. Enhancement of endocannabinoid signaling with JZL184, an inhibitor of the 2-arachidonoylglycerol hydrolyzing enzyme monoacylglycerol lipase, produces anxiolytic effects under conditions of high environmental aversiveness in rats. Pharmacol Res, 2011, 64(3): 226-234.
[4].  Guindon J, Guijarro A, Piomelli D, et al. Peripheral antinociceptive effects of inhibitors of monoacylglycerol lipase in a rat model of inflammatory pain. Br J Pharmacol, 2011, 163(7): 1464-1478.

Chemical Properties

Cas No. 1101854-58-3 SDF
化学名 (4-nitrophenyl) 4-[bis(1,3-benzodioxol-5-yl)-hydroxymethyl]piperidine-1-carboxylate
Canonical SMILES C1CN(CCC1C(C2=CC3=C(C=C2)OCO3)(C4=CC5=C(C=C4)OCO5)O)C(=O)OC6=CC=C(C=C6)[N+](=O)[O-]
分子式 C27H24N2O9 分子量 520.49
溶解度 ≥ 20.35mg/mL in DMSO 储存条件 Store at -20°C
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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。
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1 mM 1.9213 mL 9.6063 mL 19.2127 mL
5 mM 0.3843 mL 1.9213 mL 3.8425 mL
10 mM 0.1921 mL 0.9606 mL 1.9213 mL
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