JZP-361

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

JZP-361是一种有效的、可逆的、选择性的人重组 MAGL (hMAGL) 抑制剂，IC50 为 46 nM。JZP-361 还具有抗组胺能活性，可用于哮喘的研究。

JZP-361 is a potent, reversible and selective inhibitor of human recombinant MAGL (hMAGL) with an IC50 of 46 nM. JZP-361 also shows antihistaminergic activities and can be used for asthma research.

JZP-361 has almost 150-fold higher selectivity over human recombinant fatty acid amide hydrolase (hFAAH, IC50 = 7.24 μM) and 35-fold higher selectivity over human α/β-hydrolase-6 (hABHD6, IC50 = 1.79 μM).JZP-361 retains H1 antagonistic affinity (pA2 = 6.81) but did not show cannabinoid receptor activity, when tested at concentrations ≤10 μM.JZP-361 displays favorable interactions within the active site of hMAGL including the important hydrogen-bonding of the carbonyl oxygen to the oxyanion hole.

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Metabolic Enzyme/Protease

Lipase

Lipase

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1680193-80-9

405.88

C22H20ClN5O

>98% (HPLC)

In Vitro:?DMSO 中的溶解度 : 125 mg/mL (307.97 mM; 超声助溶 (<60°C)

Clc1ccc2c(CCc3cccnc3C2=C2CCN(CC2)C(=O)n2cncn2)c1

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(-20℃)

With Ice Pack

≥ 2 years