JZP 361

Names

[ CAS No. ]:
1680193-80-9

[ Name ]:
JZP 361

[Synonym ]:
[4-(8-Chloro-5,6-dihydro-11H-benzo[5,6]cyclohepta[1,2-b]pyridin-11-ylidene)-1-piperidinyl](1H-1,2,4-triazol-1-yl)methanone
Methanone, [4-(8-chloro-5,6-dihydro-11H-benzo[5,6]cyclohepta[1,2-b]pyridin-11-ylidene)-1-piperidinyl]-1H-1,2,4-triazol-1-yl-

Biological Activity

[Description]:

JZP-361 is a potent and reversible inhibitor of human recombinant MAGL (hMAGL, IC50=46 nM), and 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 represents a dual-acting pharmacological tool possessing both MAGL inhibitory and antihistaminergic activities[1].

[Related Catalog]:

Signaling Pathways >> Immunology/Inflammation >> Histamine Receptor
Signaling Pathways >> Metabolic Enzyme/Protease >> MAGL
Research Areas >> Inflammation/Immunology
Signaling Pathways >> GPCR/G Protein >> Histamine Receptor

[Target]

H1 Receptor:6.81 (pA2)


[References]

[1]. Jayendra Z Patel, et al. Loratadine analogues as MAGL inhibitors. Bioorg Med Chem Lett. 2015 Apr 1;25(7):1436-42.

Chemical & Physical Properties

[ Density]:
1.4±0.1 g/cm3

[ Boiling Point ]:
611.7±65.0 °C at 760 mmHg

[ Molecular Formula ]:
C22H20ClN5O

[ Molecular Weight ]:
405.880

[ Flash Point ]:
323.8±34.3 °C

[ Exact Mass ]:
405.135651

[ LogP ]:
3.88

[ Vapour Pressure ]:
0.0±1.8 mmHg at 25°C

[ Index of Refraction ]:
1.725

Related Compounds