1962928-26-2

BGC 20-1531 is a potent and selective antagonist of the prostaglandin E₂ (PGE₂; ) receptor subtype 4 (EP₄) with K_i values of 11.7, >10,000, and >10,000 nM for EP₄, EP₂, and EP₃, respectively. It is selective for EP₄, exhibiting <50% inhibition at 47 ion channels, cell-surface transporters, enzymes, and nuclear receptors at a concentration of 10 μM. BGC 20-1531 antagonizes PGE₂-induced cAMP accumulation in a dose-dependent manner in HEK293 EBNA cells that stably express human EP₄ receptors. It also reverses PGE₂-induced vasorelaxation (K_b = 15.85 nM) in human middle cerebral and middle meningeal arterial rings. BGC 20-1531 prevents PGE₂-induced increases in carotid blood flow and decreases in carotid resistance with an ID₅₀ value of 5 mg/kg in dogs.

BGC 20-1531 Hydrochloride, is a potent and selective EP4 antagonist, exhibiting <50% inhibition at 47 ion channels, cell-surface transporters, enzymes, and nuclear receptors at a concentration of 10 μM. It also Inhibits PGE2-induced vasodilation of middle cerebral and meningeal arterieshuman middle cerebral and middle meningeal arterial rings.

Desiccate at RT

[1] KA MAUBACH. BGC20-1531, a novel, potent and selective prostanoid EP4 receptor antagonist: a putative new treatment for migraine headache[J]. British Journal of Pharmacology, 2009, 156 2: 316-327. DOI: 10.1111/j.1476-5381.2009.00027.x