892664-04-9

892664-04-9 structure

Name: GSK-269984A
Chemical Name: sodium,6-[[5-chloro-2-[(4-chloro-2-fluorophenyl)methoxy]phenyl]methyl]pyridine-2-carboxylate
CAS Number: 892664-04-9
Molecular Formula: C₂₀H₁₄Cl₂FNNaO₃
Molecular Weight: 429.22
Catalog: Signaling Pathways GPCR/G Protein Prostaglandin Receptor
Create Date: 2016-05-29 16:13:14
Modify Date: 2024-01-02 21:33:19
GSK-269984A is a Prostaglandin E2 Receptor 1 (EP1) antagonist with a pIC50 of 7.9.

Name	sodium,6-[[5-chloro-2-[(4-chloro-2-fluorophenyl)methoxy]phenyl]methyl]pyridine-2-carboxylate
Synonyms	GSK-269984A

Description	GSK-269984A is a Prostaglandin E2 Receptor 1 (EP1) antagonist with a pIC50 of 7.9.
Related Catalog	Signaling Pathways >> GPCR/G Protein >> Prostaglandin Receptor Research Areas >> Neurological Disease
Target	EP1 Receptor:7.9 (pIC50)
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 ratand dog and high clearance in the monkey which is reflected in the half-life for each species[1].
Animal Admin	Rats are used in this study. GSK-269984A is progressed to the rat CFA model of inflammatory pain. GSK-269984A is dosed orally at doses of 1, 3 and 10 mg/kg, 23 h after intraplantar administration of the adjuvant. Analgesia is assessed 1 h post-dose of GSK-269984A[1].
References	[1]. Hall A, et al. Discovery of sodium 6-[(5-chloro-2-{[(4-chloro-2-fluorophenyl)methyl]oxy}phenyl)methyl]-2-pyridinecarboxylate (GSK269984A) an EP(1) receptor antagonist for the treatment of inflammatory pain. Bioorg Med Chem Lett. 2009 May 1;19(9):2599-603.