| Identification | Back Directory | [Name]
GSK726701A | [CAS]
945721-87-9 | [Synonyms]
GSK726701A
GSK-726701A,GSK726701A
Benzeneacetic acid, 4-(4,9-diethoxy-1,3-dihydro-1-oxo-2H-benz[f]isoindol-2-yl)-2-fluoro- | [Molecular Formula]
C24H22FNO5 | [MDL Number]
MFCD31746882 | [MOL File]
945721-87-9.mol | [Molecular Weight]
423.43 |
| Hazard Information | Back Directory | [Description]
GSK726701A is a novel prostaglandin E2 receptor 4 (EP4) partial agonist with a pEC50 of 7.4. 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 (pEC50=8.2) in a human whole blood (HWB) assay on the inhibition of LPS-mediated TNFα induction[1]. 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 ED50 of 0.2mg/kg in the FCA acute rat model of inflammatory pain[1]. | [References]
[1]. Healy MP, et al. Discovery of {4-[4,9-bis(ethyloxy)-1-oxo-1,3-dihydro-2H-benzo[f]isoindol-2-yl]-2-fluorophenyl}acetic acid (GSK726701A), a novel EP4 receptor partial agonist for the treatment of pain. Bioorg Med Chem Lett. 2018 Jun 1;28(10):1892-1896. |
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