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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产品名称 | Lipase ↓ ↑ | 其他靶点 | 纯度 | ||||||||||||||||
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XEN445 |
+++
endothelial lipase, IC50: 0.237 μM |
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JZL184 |
++++
MAGL, IC50: 8 nM |
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Tanshinone IIA | ✔ | {[allProObj[0].p_purity_real_show]} | |||||||||||||||||
Orlistat | ✔ | {[allProObj[0].p_purity_real_show]} | |||||||||||||||||
Atglistatin |
++
ATGL, IC50: 0.7 μM |
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1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多,抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用,但抑制强度暂时没有相关数据。 |
靶点 |
|
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]. |
细胞系 | 浓度 | 检测类型 | 检测时间 | 活动说明 | 数据源 |
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 |
计算器 | ||||
存储液制备 | 1mg | 5mg | 10mg | |
1 mM 5 mM 10 mM |
1.92mL 0.38mL 0.19mL |
9.61mL 1.92mL 0.96mL |
19.21mL 3.84mL 1.92mL |
CAS号 | 1101854-58-3 |
分子式 | C27H24N2O9 |
分子量 | 520.49 |
别名 | |
运输 | 蓝冰 |
存储条件 |
粉末 Sealed in dry,2-8°C 液体 -20°C:3-6个月-80°C:12个月 |
溶解度 |
DMSO: 35 mg/mL(67.24 mM),注意:DMSO长时间开封后,会吸水并导致溶解能力下降,请避免使用长期开封的DMSO |
动物实验配方 |
5%DMSO+40%PEG300+5%Tween80+water 2.5 mg/mL |