tcsc0003376 GSK-269984A

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Product Description

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].


CAS No892664-04-9
Clinical Informationclinicalinformation
PathwayGPCR/G Protein
TargetProstaglandin Receptor


Purity / Grade>98%
Solubility10 mM in DMSO

Misc Information

Observed Molecular Weight429.22
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