GSK-269984A is a Prostaglandin E2 Receptor 1 (EP1) antagonist with a pIC 50 of 7.9.
性状
Solid
IC50 & Target[1][2]
pIC50: 7.9 (Prostaglandin E2 Receptor 1 (EP1))
体外研究(In Vitro)
Results from [H]-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. has not independently confirmed the accuracy of these methods. They are for reference only.
体内研究(In Vivo)
GSK-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
and dog and high clearance in the monkey which is reflected in the half-life for each species. has not independently confirmed the accuracy of these methods. They are for reference only.
运输条件
Room temperature in continental US; may vary elsewhere.
储存方式
Powder -20°C 3 years;4°C 2 years
参考文献
[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.
溶解度数据
In Vitro: DMSO : 7 mg/mL (16.31 mM; ultrasonic and warming and heat to 60°C)配制储备液