AMG 837 calcium hydrate

SKU: orb1296266

Description

AMG 837 calcium hydrate

Research Area

Product Categories/Products/Small Molecules,Endocrinology/Hormones|||GPCR/G Protein

Key Properties

• CAS Number: 1259389-38-2
• MW: 950.97
• Purity: 98.07%
• Formula: C₅₂H₄₈CaF₆O₈
• 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]

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 .

Storage & Handling

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

Compound Identifiers

PubChem CID

154584011