JZL184

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

JZL 184 是一种有效的选择性 MAGL 抑制剂，抑制小鼠脑膜中的 MAGL 和 FAAH 的 IC50 分别为 8 nM 和 4 μM。

JZL184 is highly selective, and potent MAGL inhibitor ( monoacylglycerol lipase inhibitor). JZL184 improves behavior and neural properties in Ts65Dn mice, a model of down syndrome. JZL184 attenuates LPS-induced increases in cytokine expression in the rat frontal cortex and plasma: differential mechanisms of action. JZL184 also suppresses inflammatory pain in the mouse carrageenan model.

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.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. Animal Model:Male C57Bl/6 mice (6-8 weeks old, 20-26 g) Dosage:4 mg/kg, 8 mg/kg, 16 mg/kg, 40 mg/kg Administration:Intraperitoneal injection; once Result:Produced a rapid and sustained blockade of brain 2-AG hydrolase activity in mice, resulting in 8-fold elevations in endogenous 2-AG levels that were maintained for at least 8 h.

JZL184 | JZL 184 | JZL-184

Others

Other Targets

MAGL

Neurological Disease

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1101854-58-3

520.49

C27H24N2O9

>98% (HPLC)

DMSO : ≥ 35 mg/mL; 67.24 mM

OC(C1CCN(CC1)C(=O)Oc1ccc(cc1)[N+](=O)[O-])(c1ccc2OCOc2c1)c1ccc2OCOc2c1

4-nitrophenyl 4-(bis(benzo[d][1,3]dioxol-5-yl)(hydroxy)methyl)piperidine-1-carboxylate.

(-20℃)

With Ice Pack

≥ 2 years