Description
AMG 837 hemicalcium is a potent, orally bioavailable and partial agonist of GPR40/FFA1. AMG 837 hemicalcium inhibits specific [3H]AMG 837 binding at the human FFA1 receptor with a pIC50 of 8.13. AMG 837 hemicalcium could enhance insulin secretion and lower glucose levels in rodents.
Product information
CAS Number: 1291087-14-3
Molecular Weight: 457.47
Formula: C52H40CaF6O6
Chemical Name: calcium bis((3S)-3-(4-{[4'-(trifluoromethyl)-[1,1'-biphenyl]-3-yl]methoxy}phenyl)hex-4-ynoate)
Smiles: [Ca+2].CC#C[C@@H](CC([O-])=O)C1C=CC(=CC=1)OCC1=CC(=CC=C1)C1C=CC(=CC=1)C(F)(F)F.CC#C[C@@H](CC([O-])=O)C1C=CC(=CC=1)OCC1=CC(=CC=C1)C1C=CC(=CC=1)C(F)(F)F
InChiKey: WCZAHGONZBHQSA-HRQBZJEISA-L
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
Technical Data
Appearance: Solid Power
Purity: ≥98% (or refer to the Certificate of Analysis)
Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis
Storage Condition: Dry, dark and -20 oC for 1 year or refer to the Certificate of Analysis.
Shelf Life: ≥12 months if stored properly.
Stock Solution Storage: 0 - 4 oC for 1 month or refer to the Certificate of Analysis.
Drug Formulation: To be determined
HS Tariff Code: 382200
How to use
In Vitro:
AMG 837 (1 nM-10 μM) stimulates insulin secretion in a glucose-dependent manner with an EC50 of 142±20 nM on islets isolated from mice. AMG 837 stimulates Ca2+ flux with the EC50s of 13.5, 22.6 and 31.7 nM for human, mouse and rat receptors in CHO cells, respectively.
In Vivo:
AMG 837 (0.03-0.3 mg/kg; a single p.o.) improves glucose tolerance and enhances insulin secretion in Sprague-Dawley rats. AMG 837 (0.03-0.3 mg/kg; p.o. once daily for 21 days) reduces glucose levels and increases insulin levels following glucose challenge in vivo. AMG 837 (0.5 mg/kg; p.o.) displays excellent oral bioavailability (F = 84%) and a total plasma Cmax of 1.4 µM.
Products are for research use only. Not for human use.
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