GSK-269984A (C09-1135-726)

GSK-269984A is a Prostaglandin E2 Receptor 1 (EP1) antagonist with a pIC 50 of 7.9.In VitroResults from [ 3 H]-PGE 2 binding assay in CHO cells overexpressing the human EP 1 receptor demonstrate that GSK-269984A is an antagonist of EP 1 receptor with a pIC 50 of 7.9. GSK-269984A is found to cause a concentration-dependent rightward shift of the PGE 2 dose-response curve and Schild analysis shows that GSK-269984A is a competitive antagonist with pA 2 8.1±0.3 and slope 1.0. MCE has not independently confirmed the accuracy of these methods. They are for reference only.In VivoGSK-269984A demonstrates an ED 50 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/nand dog and high clearance in the monkey which is reflected in the half-life for each species . MCE has not independently confirmed the accuracy of these methods. They are for reference only.Form:SolidIC50& Target:EP1 7.9 (pIC 50 ). Specification: 0.99 Molecular Formula: C20H14Cl2FNNaO3 Molecular Weight: 429.22 PubChem CID: 23696973 Isomeric SMILES: C1=CC(=NC(=C1)C(=O)[O-])CC2=C(C=CC(=C2)Cl)OCC3=C(C=C(C=C3)Cl)F.[Na+]