JZL184 |
| Catalog No.GC14390 |
JZL184는 뇌막(8 nM의 IC50)에서 2-아라키도노일글리세롤(2-AG) 가수분해를 차단하는 강력하고 선택적이고 비가역적인 MAGL 억제제입니다.
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Cas No.: 1101854-58-3
Sample solution is provided at 25 µL, 10mM.
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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.
| Cas No. | 1101854-58-3 | SDF | |
| Chemical Name | (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-] | ||
| Formula | C27H24N2O9 | M.Wt | 520.49 |
| Solubility | ≥ 20.35mg/mL in DMSO | Storage | Store at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
||
| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
|
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 |
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Quality Control & SDS
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- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
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Average Rating: 5 (Based on Reviews and 3 reference(s) in Google Scholar.)
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