For research use only. Not for therapeutic Use.
KAG-308 is a potent selective and orally active agonist of EP4 receptor (a prostaglandin E2 receptor subtype), suppresses colitis and promotes histological mucosal healing, potently inhibits TNF-α production. KAG-308 shows a Ki and an EC50 of 2.57 nM and 17 nM for human EP4 receptor, respectively, more selective over EP1, EP2, EP3 and IP receptor[1].
KAG-308 is a potent selective and orally active agonist of EP4 receptor, suppresses colitis and promots histological mucosal healing. KAG-308 shows a Ki and EC50 values of 2.57 nM and 17 nM for human EP4 receptor, respectively, more selective over human EP1 (Ki, 1410 nM; EC50, 1000 nM), EP2 (Ki, 1540 nM; EC50, 1000 nM), EP3 (Ki, 32.4 nM; EC50, 160 nM) and IP receptor (Ki, 52.9 nM; EC50, >10000 nM). KAG-308 also exhibits potent agonist activity for human and mouse EP4 with an EC50 of 0.15 nM and 1.0 nM, respectively in the dual luciferase reporter assay[1].
| Catalog Number | I018953 |
| CAS Number | 1215192-68-9 |
| Synonyms | (2Z,3aR,4R,5R,6aS)-3,3-difluoro-4-[(E,3R,4R)-3-hydroxy-4-(3-methylphenyl)pent-1-enyl]-2-[4-(2H-tetrazol-5-yl)butylidene]-4,5,6,6a-tetrahydro-3aH-cyclopenta[b]furan-5-ol |
| Molecular Formula | C24H30F2N4O3 |
| Purity | ≥95% |
| InChI | InChI=1S/C24H30F2N4O3/c1-14-6-5-7-16(12-14)15(2)18(31)11-10-17-19(32)13-20-23(17)24(25,26)21(33-20)8-3-4-9-22-27-29-30-28-22/h5-8,10-12,15,17-20,23,31-32H,3-4,9,13H2,1-2H3,(H,27,28,29,30)/b11-10+,21-8-/t15-,17+,18-,19-,20+,23-/m1/s1 |
| InChIKey | KSELABKNBIUMGG-YGBAREPYSA-N |
| SMILES | CC1=CC(=CC=C1)C(C)C(C=CC2C(CC3C2C(C(=CCCCC4=NNN=N4)O3)(F)F)O)O |
| Reference | [1]. Watanabe Y, et al. KAG-308, a newly-identified EP4-selective agonist shows efficacy for treating ulcerative colitis and can bring about lower risk of colorectal carcinogenesis by oral administration. Eur J Pharmacol. 2015 May 5;754:179-89. |
