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Submit ReviewAMG 837 hemicalcium salt is a 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 (Cat. No. 3687). Potentiates glucose-dependent stimulation of insulin in vivo. Antidiabetic.
AMG 837 hemicalcium salt is also offered as part of the Tocriscreen 2.0 Max. 了解 Tocris 化合物库的更多信息。
分子量 | 457.47 |
公式 | C26H20F3O3.½Ca |
储存 | Store at +4°C |
纯度 | ≥98% (HPLC) |
CAS Number | 1291087-14-3 |
PubChem ID | 46854655 |
InChI Key | WCZAHGONZBHQSA-UHFFFAOYSA-L |
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] |
上方提供的技术数据仅供参考。批次相关数据请参见分析证书。
Tocris products are intended for laboratory research use only, unless stated otherwise.
溶剂 | 最高浓度 mg/mL | 最高浓度 mM | |
---|---|---|---|
溶解性 | |||
DMSO | 45.75 | 100 |
以下数据基于产品分子量 457.47。 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
浓度/溶剂体积/质量 | 1 mg | 5 mg | 10 mg |
---|---|---|---|
1 mM | 2.19 mL | 10.93 mL | 21.86 mL |
5 mM | 0.44 mL | 2.19 mL | 4.37 mL |
10 mM | 0.22 mL | 1.09 mL | 2.19 mL |
50 mM | 0.04 mL | 0.22 mL | 0.44 mL |
参考文献是支持产品生物活性的出版物。
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
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