AMG 837 hemicalcium salt 是一种有效的、口服生物可利用的 GPR40/FFA1 部分激动剂。
| Cas No. | 1291087-14-3 |
| Canonical SMILES | CC#C[C@H](C1=CC=C(C=C1)OCC2=CC=CC(C3=CC=C(C(F)(F)F)C=C3)=C2)CC([O-])=O.CC#C[C@H](C4=CC=C(C=C4)OCC5=CC=CC(C6=CC=C(C(F)(F)F)C=C6)=C5)CC([O-])=O.[Ca+2] |
| 分子式 | C26H20F3O3.½Ca |
| 分子量 | 457.47 |
| 溶解度 | Soluble in DMSO |
| 储存条件 | Store at -20°C |
| General tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while. |
| Shipping Condition | Evaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request |
| 产品描述 | Potent free fatty acid receptor 1 (FFA1/GPR40) partial agonist (EC50 values are 13.5, 22.6 and 31.7 nM at human, mouse and rat receptors, respectively). Interacts allosterically with full FFA1 agonist Docosahexaenoic acid . Potentiates glucose-dependent stimulation of insulin in vivo. Antidiabetic. Houze et al (2012) AMG 837: a potent, orally bioavailable GPR40 agonist. Bioorg.Med.Chem.Lett. 22 1267 PMID:22217876 |Lin et al (2012) Identification and pharmacological characterization of multiple allosteric binding sites on the free fatty acid 1 receptor. Mol.Pharmacol. 82 843 PMID:22859723 |Lin et al (2011) AMG 837: a novel GPR40/FFA1 agonist that enhances Ins secretion and lowers glucose levels in rodents. PLoS One 6 e27270 PMID:22087278 |
