WARNING: This product is for research use only, not for human or veterinary use.
MedKoo CAT#: 555436
Description: BAY-1316957 is a highly potent, selective, orally available human prostaglandin E2 receptor subtype 4 (hEP4-R) antagonist (IC50= 15.3 nM ) with excellent drug metabolism and pharmacokinetics properties. Notably, treatment with BAY 1316957 can be expected to lead to prominent and rapid pain relief and significant improvement of the patient’s quality of life.
MedKoo Cat#: 555436
Chemical Formula: C27H27N3O3
Exact Mass: 441.2052
Molecular Weight: 441.531
Elemental Analysis: C, 73.45; H, 6.16; N, 9.52; O, 10.87
Synonym: BAY-1316957; BAY 1316957; BAY1316957;
IUPAC/Chemical Name: 2-(9-Ethyl-6-methyl-9H-carbazol-3-yl)-1-(2-methoxyethyl)-4-methyl-1H-benzimidazole-5-carboxylic acid
InChi Key: FHXIZAPGGULPIK-UHFFFAOYSA-N
InChi Code: InChI=1S/C27H27N3O3/c1-5-29-22-9-6-16(2)14-20(22)21-15-18(7-10-23(21)29)26-28-25-17(3)19(27(31)32)8-11-24(25)30(26)12-13-33-4/h6-11,14-15H,5,12-13H2,1-4H3,(H,31,32)
SMILES Code: O=C(C1=CC=C2C(N=C(C3=CC4=C(C=C3)N(CC)C5=C4C=C(C)C=C5)N2CCOC)=C1C)O
The presence and growth of endometrial tissue outside the uterine cavity in endometriosis patients are primarily driven by hormone-dependent and inflammatory processesthe latter being frequently associated with severe, acute, and chronic pelvic pain. The EP4 subtype of prostaglandin E2 (PGE2) receptors (EP4-R) is a particularly promising antiinflammatory and antinociceptive target as both this receptor subtype and the pathways forming PGE2 are highly expressed in endometriotic lesions.
Identification of a Benzimidazolecarboxylic Acid Derivative (BAY 1316957) as a Potent and Selective Human Prostaglandin E2 Receptor Subtype 4 (hEP4-R) Antagonist for the Treatment of Endometriosis
Stefan Bäurle, Jens Nagel, Olaf Peters, Nico Bräuer, Antonius ter Laak, Cornelia Preusse, Antje Rottmann, Dieter Heldmann, Ulrich Bothe, Thorsten Blume, Ludwig Zorn, Daryl Walter, Thomas M. Zollner, Andreas Steinmeyer, and Gernot Langer
Publication Date (Web): February 1, 2019 (Article)