For research use only. Not for therapeutic Use.
Orally bioavailable partial agonist of the GPR40 (EC50 value 13.5 nM for AMG 837 stimulated Ca2+ flux in CHO cells expressing human GPR40) with a superior pharmacokinetic profile. AMG837 stimulated robust glucose-dependent insulin secretion (EC50 value 142±20 nM) in isolated rodent islets, and lowered post-prandial glucose in normal rats. AMG-837 exhibits a potential utility for the treatment of type 2 diabetes.
| Catalog Number | I011372 |
| CAS Number | 1291087-14-3 |
| Molecular Formula | C26H20F3O3.0.5Ca |
| Purity | ≥95% |
| IUPAC Name | calcium;(3S)-3-[4-[[3-[4-(trifluoromethyl)phenyl]phenyl]methoxy]phenyl]hex-4-ynoate |
| InChI | InChI=1S/2C26H21F3O3.Ca/c2*1-2-4-21(16-25(30)31)20-9-13-24(14-10-20)32-17-18-5-3-6-22(15-18)19-7-11-23(12-8-19)26(27,28)29;/h2*3,5-15,21H,16-17H2,1H3,(H,30,31);/q;;+2/p-2/t2*21-;/m00./s1 |
| SMILES | CC#C[C@@H](CC(=O)[O-])C1=CC=C(C=C1)OCC2=CC(=CC=C2)C3=CC=C(C=C3)C(F)(F)F.CC#C[C@@H](CC(=O)[O-])C1=CC=C(C=C1)OCC2=CC(=CC=C2)C3=CC=C(C=C3)C(F)(F)F.[Ca+2] |
| Reference | D.C. Lin et al. AMG 837: a novel GPR40/FFA1 agonist that enhances insulin secretion and lowers glucose levels in rodents. PLoS One. 2011;6(11):e27270.
J.B. Houze et al. AMG 837: a potent, orally bioavailable GPR40 agonist. Bioorg Med Chem Lett. 2012 Jan 15;22(2):1267-70.
J. Luo et al. A potent class of GPR40 full agonists engages the enteroinsular axis to promote glucose control in rodents. PLoS One. 2012;7(10):e46300.
Y.J. Choi et al. G-protein coupled receptor 40 agonists as novel therapeutics for type 2 diabetes. Arch Pharm Res. 2014 Apr;37(4):435-9. |
