JZL184
目录号 : GC14390
A potent and selective inhibitor of MAGL
Cas No.:1101854-58-3
Sample solution is provided at 25 µL, 10mM.
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Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
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.
| 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 |
| 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 | 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 |
| 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。