For research use only. Not for therapeutic Use.
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].
| Catalog Number | I019717 |
| CAS Number | 945721-87-9 |
| Synonyms | 2-[4-(4,9-diethoxy-3-oxo-1H-benzo[f]isoindol-2-yl)-2-fluorophenyl]acetic acid |
| Molecular Formula | C24H22FNO5 |
| Purity | ≥95% |
| InChI | InChI=1S/C24H22FNO5/c1-3-30-22-16-7-5-6-8-17(16)23(31-4-2)21-18(22)13-26(24(21)29)15-10-9-14(11-20(27)28)19(25)12-15/h5-10,12H,3-4,11,13H2,1-2H3,(H,27,28) |
| InChIKey | YJEFCZJZEASKIO-UHFFFAOYSA-N |
| SMILES | CCOC1=C2CN(C(=O)C2=C(C3=CC=CC=C31)OCC)C4=CC(=C(C=C4)CC(=O)O)F |
| Reference | [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. |
