GSK726701A (C09-1135-729)

GSK726701A is a novel prostaglandin E2 receptor 4 (EP4) partial agonist with a pEC 50 of 7.4.In VitroGSK726701A 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 VivoGSK726701A 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.Form:SolidIC50& Target:pEC50: 7.4. Specification: 0.98 Molecular Formula: C24H22FNO5 Molecular Weight: 423.43 PubChem CID: 16678098 Isomeric SMILES: CCOC1=C2CN(C(=O)C2=C(C3=CC=CC=C31)OCC)C4=CC(=C(C=C4)CC(=O)O)F