GSK726701A

小分子

GSK726701A

G656649-1ml

1ml

10mM in DMSO

-80℃储存

超低温冰袋运输

GSK726701A is a novel prostaglandin E2 receptor 4 (EP4) partial agonist with a pEC 50 of 7.4. In Vitro GSK726701A has high selectivity (>100-fold) against a set of other prostaglandin receptors (EP1-3 , DP1 , FP, IP, TP) and no significant activity against a wider panel of targets. It demonstrates EP4 agonist activity with similar potency and intrinsic activity (pEC 50 =8.2) in a human whole blood (HWB) assay on the inhibition of LPS-mediated TNFα induction. MCE has not independently confirmed the accuracy of these methods. They are for reference only. In Vivo GSK726701A has good pharmacokinetic file in rat, dog and monkey. GSK726701A has robust activity in a range of animal models of inflammatory and neuropathic pain GSK726701A demonstrates a time-dependant, full reversal of CCI-induced mechanical allodynia at 3mg/kg, equivalent to the clinical gold standard gabapentin (30mg/kg). GSK726701A has an ED 50 of 0.2mg/kg in the FCA acute rat model of inflammatory pain . MCE has not independently confirmed the accuracy of these methods. They are for reference only. IC50& Target:pEC50: 7.4

GSK726701A 是一种新型前列腺素 E2 受体 4 (EP4) 部分激动剂，pEC 50 为 7.4。

945721-87-9(DMSO)

C24H22FNO5

423.43 g/mol

CCOC1=C2CN(C(=O)C2=C(C3=CC=CC=C31)OCC)C4=CC(=C(C=C4)CC(=O)O)F