For research use only. Not for therapeutic Use.
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].
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].
| Catalog Number | I011226 |
| CAS Number | 1680193-80-9 |
| Synonyms | [4-(13-chloro-4-azatricyclo[9.4.0.03,8]pentadeca-1(11),3(8),4,6,12,14-hexaen-2-ylidene)piperidin-1-yl]-(1,2,4-triazol-1-yl)methanone |
| Molecular Formula | C22H20ClN5O |
| Purity | ≥95% |
| InChI | InChI=1S/C22H20ClN5O/c23-18-5-6-19-17(12-18)4-3-16-2-1-9-25-21(16)20(19)15-7-10-27(11-8-15)22(29)28-14-24-13-26-28/h1-2,5-6,9,12-14H,3-4,7-8,10-11H2 |
| InChIKey | GAVZCGTYRWKKDV-UHFFFAOYSA-N |
| SMILES | C1CC2=C(C=CC(=C2)Cl)C(=C3CCN(CC3)C(=O)N4C=NC=N4)C5=C1C=CC=N5 |
| Reference | [1]. Jayendra Z Patel, et al. Loratadine analogues as MAGL inhibitors. Bioorg Med Chem Lett. 2015 Apr 1;25(7):1436-42. |
