[TaiClone] GSK-269984A

[TaiClone] GSK-269984A

 

 

 

tcsc0003376

Specifications

Purity / Grade

>98%

 

Solubility

10 mM in DMSO

 

Smiles

smiles

Misc Information

Observed Molecular Weight

429.22

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].

Information

CAS No

892664-04-9

 

Formula

C20H14Cl2FNNaO3

 

Clinical Information

clinical

 

information

 

Pathway

 

GPCR/G Protein

 

Target

 

Prostaglandin Receptor