AMG 837 calcium hydrate

SKU: orb1296266

Description

AMG 837 calcium hydrate is a potent and selective GPR40 agonist (EC50 = 13 nM), exhibiting over 1000-fold selectivity against related receptors GPR41, GPR43, and GPR120. This small molecule is a valuable research tool for investigating GPR40's role in glucose homeostasis and insulin secretion in both cellular and animal models of diabetes.

Research Area

Metabolism Research, Pharmacology & Drug Discovery

Key Properties

• CAS Number: 1259389-38-2
• MW: 950.97
• Purity: 98.96% (May vary between batches)
• Formula: C₅₂H₄₄CaF₆O₈
• SMILES: [H]O[H].[H]O[H].O=C([O-])C[C@H](C#CC)C1=CC=C(OCC2=CC(C3=CC=C(C(F)(F)F)C=C3)=CC=C2)C=C1.O=C([O-])C[C@H](C#CC)C4=CC=C(OCC5=CC(C6=CC=C(C(F)(F)F)C=C6)=CC=C5)C=C4.[Ca+2]
• Target: GPCR
• Solubility: DMSO:40 mg/mL (42.06 mM)

Bioactivity

• Target IC50:
  FFA1/GPR40:13 nM (EC50)
• In Vivo:
  In rats, AMG 837 increases insulin release when glucose levels are elevated .
• In Vitro:
  GPR40 agonist AMG 837 displayed the expected two-fold increase in potency on GPR4 (EC50: 13 nM) compared to the racemic compound and its activity crossed over to the rat and mouse forms of GPR40 (EC50s: 23/13 nM). AMG 837 was a partial agonist on GPR40 with maximal activity 85% of that shown by DHA. An external panel of 64 receptors also revealed no significant activity with the exception of weak inhibition (IC50: 3 μM) on the α2-adrenergic receptor .
  Read more...

Storage & Handling

• Storage: -20°C
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

AMG 837 calcium, AMG 837 calcium Hydrate, AMG 837 calcium hydrate, Inhibitor, insulin, GPR40, glucose, FFAR, FFA1, Free Fatty Acid Receptor, inhibit

Compound Identifiers

PubChem CID

154584011