tcsc0003376 GSK-269984A

GSK-269984A is a Prostaglandin E2 Receptor 1 (EP1) antagonist with a pIC₅₀ of 7.9.

IC50 & Target: pIC50: 7.9 (Prostaglandin E2 Receptor 1 (EP1))^[1]

In Vitro: Results from [³H]-PGE₂ binding assay in CHO cells overexpressing the human EP₁ receptor demonstrate that GSK-269984A is an antagonist of EP₁ receptor with a pIC₅₀ of 7.9. GSK-269984A is found to cause a concentration-dependent rightward shift of the PGE₂ dose-response curve and Schild analysis shows that GSK-269984A is a competitive antagonist with pA₂ 8.1±0.3 and slope 1.0^[1].

In Vivo: GSK-269984A demonstrates an ED₅₀ of 2.6 mg/kg (po), with the 10 mg/kg dose showing equivalent reversal of hypersensitivity to the standard. GSK-269984A displays moderate blood clearance in the rat

and dog and high clearance in the monkey which is reflected in the half-life for each species^[1].