Metabolex-36  (Synonyms: Met-36)

Metabolex-36 is a FFA4 agonist developed by Metabolex (now Cymabay Therapeutics) and used in multiple studies to investigate the function of FFA4. Metabolex-36 was used in conjunction with AstraZeneca compounds (AZ-423 and AZ-670) to investigate FFA4 function in pancreatic delta cells. Metabolex-36 has a pEC50 of 5.9 for FFA4 and a pEC50 of less than 4.0 for FFA1. Compound B was used to investigate the role of FFA4 in growth hormone-releasing peptide (ghrelin) secretion and somatostatin release and was used with FFA4 KO mice. Compound B had an EC50 of 15 nM for FFA4 in an IP3 accumulation assay in FFA4-transfected COS7 cells and was up to 1000-fold selective for FFA1. Compound B inhibited baseline ghrelin secretion from primary gastric mucosal cells but had no effect on cells from FFA4 KO mice. Oral administration of Compound B reduced plasma ghrelin levels in mice under starvation conditions. Compound B also inhibited somatostatin release from primary gastric epithelial cells but had no effect on cells from FFA4 KO mice.

420.84

C₂₁H₁₉ClF₂N₂O₃

1224102-50-4

O=C(O)C(C)CC1=CC(F)=C(OCC2=CC(C)=NN2C3=CC=C(Cl)C=C3)C(F)=C1

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• [1]. Development of Free Fatty Acid Receptor 4 (FFA4/GPR120) Agonists in Health Science