| Bioactivity | 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[1]. | ||||||||||||
| Invitro | 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)[1].JZP-361 retains H1 antagonistic affinity (pA2 = 6.81) but did not show cannabinoid receptor activity, when tested at concentrations ≤10 μM[1].JZP-361 displays favorable interactions within the active site of hMAGL including the important hydrogen-bonding of the carbonyl oxygen to the oxyanion hole[1]. | ||||||||||||
| Name | JZP-361 | ||||||||||||
| CAS | 1680193-80-9 | ||||||||||||
| Formula | C22H20ClN5O | ||||||||||||
| Molar Mass | 405.88 | ||||||||||||
| Appearance | Solid | ||||||||||||
| Transport | Room temperature in continental US; may vary elsewhere. | ||||||||||||
| Storage |
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| Reference | [1]. Jayendra Z Patel, et al. Loratadine analogues as MAGL inhibitors. Bioorg Med Chem Lett. 2015 Apr 1;25(7):1436-42. |
JZP-361
CAS: 1680193-80-9 F: C22H20ClN5O W: 405.88
JZP-361 is a potent, reversible and selective inhibitor of human recombinant MAGL (hMAGL) with an IC50 of 46 nM. JZP-361
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