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AMG 837 calcium
Axon 2405
- Parent CAS: 865231-46-5
- Optical Purity: Optically pure
- Soluble in DMSO
- MF: C26H20F3O3.0.5Ca
- MW: 457.47
Description
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.
More Information
| Parent CAS No. | 865231-46-5 |
|---|---|
| Chemical Name | (S)-3-(4-((4'-(trifluoromethyl)biphenyl-3-yl)methoxy)phenyl)hex-4-ynoic acid hemi-calcium salt |
| SMILES | C1(C(F)(F)F)C=CC(C2C=C(COC3C=CC([C@H](CC(=O)[O-])C#CC)=CC=3)C=CC=2)=CC=1 |&1:17,r| |
| MFCD | N.A. |
| InChi | InChI=1S/C26H21F3O3/c1-2-4-21(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/h3,5-15,21H,16-17H2,1H3,(H,30,31)/p-1 |
| InChiKey | ZOPNBMMVVZRSGH-UHFFFAOYSA-M |
| CID | 91826518 |
| Short Description | GPR40 partial agonist |
References
- 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.
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