ER 819762

Discontinued Product

ER 819762 (Cat. No. 5924) has been withdrawn from sale for commercial reasons.
Description: Potent EP4 receptor antagonist; orally bioavailable
Chemical Name: (10S)-1'-[(3,5-Dimethylphenyl)methyl]-2-ethyl-5,10-dihydro-7,9-dimethoxy-10-methylspiro[1H-imidazo[1,5-b][2]benzazepine-1,4'-piperidin]-3(2H)-one
Purity: ≥98% (HPLC)

Biological Activity for ER 819762

ER 819762 is a potent EP4 receptor antagonist (IC50 = 59 nM). Suppresses EP4-mediated Th1 differentiation, Th17 cell expansion, and IL-23 secretion by activated dendritic cells. Inhibits Th1 and Th17 cytokine production, suppresses collagen- and GPI-induced arthritis in mice. Attenuates CFA-induced inflammatory pain in rats. Analgesic. Orally bioavailable.

Technical Data for ER 819762

M. Wt 489.65
Formula C30H39N3O3
Storage Store at -20°C
Purity ≥98% (HPLC)
CAS Number 1155773-15-1
PubChem ID 42596951
Smiles CCN1C(N2CC3=CC(OC)=CC(OC)=C3[C@H](C=C2C14CCN(CC4)CC5=CC(C)=CC(C)=C5)C)=O

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.

Tocris products are intended for laboratory research use only, unless stated otherwise.

References for ER 819762

References are publications that support the biological activity of the product.

Chen et al (2010) A novel antagonist of the prostaglandin E2 EP4 receptor inhibits Th1 differentiation and Th17 expansion and is orally active in arthritis models. Br.J.Pharmacol. 160 292 PMID: 20423341

Jones et al (2016) Role of EP2 and EP4 receptors in airway microvascular leak induced by prostaglandin E2. Br.J.Pharmacol. 173 992 PMID: 26639895

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Citations for ER 819762

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Currently there are no citations for ER 819762.

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