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编 号:F201022
分子式:C22H20ClN5O
分子量:405.88
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10mM*1mL in DMSO
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5mg
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10mg
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25mg
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50mg
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生物活性:
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.

体外研究:
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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