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ER 819762

Names

[ CAS No. ]:
1155773-15-1

[ Name ]:
ER 819762

[Synonym ]:
(10S)-1'-(3,5-Dimethylbenzyl)-2-ethyl-7,9-dimethoxy-10-methyl-5,10-dihydrospiro[imidazo[1,5-b][2]benzazepine-1,4'-piperidin]-3(2H)-one
ER819762
Spiro[1H-imidazo[1,5-b][2]benzazepine-1,4'-piperidin]-3(2H)-one, 1'-[(3,5-dimethylphenyl)methyl]-2-ethyl-5,10-dihydro-7,9-dimethoxy-10-methyl-, (10S)-

Biological Activity

[Description]:

ER-819762 is a novel potent, selective, orally active EP4 receptor antagonist with IC50 of 59 nM in cAMP-dependent reporter assay; inhibits EP4-stimulated Th1 differentiation, Th17 cell expansion, and IL-23 secretion by activated dendritic cells; exhibits no agonism or antagonism for the related PGE2 EP1, EP2 and EP3 receptors; suppresses Th1 and Th17 cytokine production, suppresses disease in collagen- and GPI-induced arthritis in mice, and suppresses CFA-induced inflammatory pain in rats.

[References]

References 1. Chen Q, et al. Br J Pharmacol. 2010 May;160(2):292-310. 2. Jones VC, et al. Br J Pharmacol. 2016 Mar;173(6):992-1004. View Related Products by Target Prostaglandin Receptor

Chemical & Physical Properties

[ Density]:
1.2±0.1 g/cm3

[ Boiling Point ]:
622.2±65.0 °C at 760 mmHg

[ Molecular Formula ]:
C30H39N3O3

[ Molecular Weight ]:
489.649

[ Flash Point ]:
330.1±34.3 °C

[ Exact Mass ]:
489.299133

[ LogP ]:
5.20

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

[ Index of Refraction ]:
1.625

Related Compounds