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JZP 361 是一种有效、可逆和选择性的人重组 MAGL (hMAGL) 抑制剂,IC50 为 46 nM。
Potent and selective reversible MAGL inhibitor (IC50 = 46 nM). Exhibits 35-fold and 150-fold higher selectivity over human FAAH and ABHD6, respectively (IC50 values are 1.79 and 7.24 μM, respectively). Displays affinity for H1 receptors (pA2 = 6.81). Exhibits no activity at cannabinoid receptors at 10 μM.
Patel et al (2015) Loratadine analogues as MAGL inhibitors. Bioorg.Med.Chem.Lett. 25 1436 PMID:25752982
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