|4-(双(苯并[d][1,3]dioxol-5-基)(羟基)甲基)哌啶-1-羧酸-4-硝基苯酯|CsnPharm

CAS No.: 1101854-58-3

4-Nitrophenyl 4-(bis(benzo[d][1,3]dioxol-5-yl)(hydroxy)methyl)piperidine-1-carboxylate Catalog No. CSN16301

Synonyms: JZL 184

JZL 184 is a potent and selective inhibitor of MAGL with IC50 of 8 nM and 4 μM for inhibition of MAGL and FAAH in mouse brain membranes respectively.

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生物活性

实验方案

技术信息

生物活性

描述Monoacylglycerol lipase (MAGL) is a key enzyme in the human endocannabinoid system. It is also the main enzyme responsible for the conversion of 2-arachidonoyl glycerol (2-AG) to arachidonic acid (AA), a precursor of prostaglandin synthesis. The inhibition of MAGL activity would be beneficial for the treatment of a wide range of diseases, such as inflammation, neurodegeneration, metabolic disorders and cancer^[3]. JZL 184 is a potent, selective and irreversible MAGL inhibitor that blocks 2-Arachidonoylglycerol (2-AG) hydrolysis in brain membranes (IC50 of 8 nM). JZL 184 displays >300-fold selectivity for MAGL over FAAH. JZL 184 displays IC50 values of 8 nM and 4 μM for blockade of 2-AG and oleamide (FAAH substrate) hydrolysis in brain membranes, respectively. Comparable inhibitory effects are observed with recombinant MAGL and FAAH when expressed in COS7 cells. JZL 184 (4-40 mg/kg; intraperitoneal injection; once; C57Bl/6 mice) treatment produces a rapid and sustained blockade of brain 2-AG hydrolase activity in mice, resulting in 8-fold elevations in endogenous 2-AG levels that are maintained for at least 8 h. JZL 184-treated mice shows a remarkable array of CB1-dependent behavioral effects, including analgesia, hypomotility, and hypothermia^[4]. 8 mg/kg JZL-184 significantly increased the levels of 2-AG in the auditory cortex of both Fmr1 KO and WT mice 4 h post-treatment. A reduction in the abnormally enhanced baseline gamma-band power in Fmr1 KO mice and significantly improved evoked synchronization to auditory stimuli in the gamma-band range post-JZL-184 treatment. JZL-184 treatment also ameliorated anxiety-like and hyperactivity phenotypes in Fmr1 KO mice^[5]. JZL 184 prolongs depolarization-induced suppression of excitation (DSE) in Purkinje neurons in cerebellar slices and DSE inhibition (DSI) in CA1 pyramidal neurons in hippocampal slices. JZL 184 produces greater enhancement of DSE/DSI in mouse neurons than that in rat neurons^[6].
细胞研究

Cell Data

Cell Lines	Concentration	Assay Type	Time	Activity Description	Data Sources
COS7 cells	-	Function assay	-	Inhibition of human MAGL expressed in monkey COS7 cells, IC50=0.002 μM	23455058
COS7 cells	-	Function assay	-	Inhibition of human MAGL expressed in COS7 cells using endogenous 2-AG substrate, IC50=0.002 μM	22738638

参考文献

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 1.9213 mL
- 9.6064 mL
- 19.2128 mL
- 5 mM
- 0.3843 mL
- 1.9213 mL
- 3.8426 mL
- 10 mM
- 0.1921 mL
- 0.9606 mL
- 1.9213 mL

技术信息

CAS号

1101854-58-3

储存条件

粉末: Sealed in dry,2-8°C

液体: -20°C:3-6 月 -80°C:12月

分子式

C27H24N2O9

运输

蓝冰

分子量

520.49

别名

JZL 184

溶解度

DMSO	100.0 mg/mL (192.1 mM)
Water	Insoluble
Ethanol	Insoluble

动物实验配方

5%DMSO+40%PEG300+5%Tween80+water

2.5 mg/mL

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4-Nitrophenyl 4-(bis(benzo[d][1,3]dioxol-5-yl)(hydroxy)methyl)piperidine-1-carboxylate Catalog No. CSN16301

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