GSK-269984A is aProstaglandin E2 Receptor 1 (EP1)antagonist with apIC₅₀of 7.9.

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

Results from [³H]-PGE₂binding assay in CHO cells overexpressing the human EP₁receptor demonstrate that GSK-269984A is an antagonist of EP₁receptor with a pIC₅₀of 7.9. GSK-269984A is found to cause a concentration-dependent rightward shift of the PGE₂dose-response curve and Schild analysis shows that GSK-269984A is a competitive antagonist with pA₂8.1±0.3 and slope 1.0^[1].

GSK-269984A demonstrates an ED₅₀of 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].

429.22

Solid

C₂₀H₁₄Cl₂FNNaO₃

892664-04-9

Room temperature in continental US; may vary elsewhere.

DMSO : 7 mg/mL(16.31 mM;ultrasonic and warming and heat to 60℃)

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