AMG7703

• CAT Number: I002119
• CAS Number: 1103523-24-5
• Molecular Formula: C14H15ClN2OS
• Molecular Weight: 294.80
• Purity: ≥95%
• Synonyms: (2S)-2-(4-chlorophenyl)-3-methyl-N-(1,3-thiazol-2-yl)butanamide
• InChI: InChI=1S/C14H15ClN2OS/c1-9(2)12(10-3-5-11(15)6-4-10)13(18)17-14-16-7-8-19-14/h3-9,12H,1-2H3,(H,16,17,18)/t12-/m0/s1
• InChIKey: AZYDQCGCBQYFSE-LBPRGKRZSA-N
• SMILES: CC(C)C(C1=CC=C(C=C1)Cl)C(=O)NC2=NC=CS2

AMG7703 is a selective and allosteric agonists of FFA2 (GPR43), the receptor for short-chain fatty acids (SCFAs), acetate, and propionate. AMG7703 can be used to research for in inflammatory and metabolic[1].
AMG7703 (phenylacetamide 1) (30 μM) shows selectivity on FFA2 (GPR43) over FFA1 (GPR40) and FFA3 (GPR41) with in Chinese hamster ovary cells[1].
AMG7703 (0.041, 0.123, 0.37, 1.11 μM) acts as an FFA2 allosteric agonist, activates Gαi coupled signaling pathway[1].
AMG7703 (1, 3, 10, 30 μM) results in Gαi-dependent inhibition of lipolysis in adipocytes (3T3L1)[1].
AMG7703 (0.041, 0.123, 0.37, 1.11 μM) exhibits allosteric activity and inhibits Gαi-coupled cAMP with IC50 values of 0.7 μM (hFFA2) and 0.96 μM (mFFA2), respectively; as for Gαq-coupled aequorin inhibition, with EC50s of 0.45 μM (hFFA2) and 1.27 μM (mFFA2), respectively[1].
AMG7703 (0-1 μM) shows the positive cooperating effect of acetate and stimulates calcium mobilization in a concentration-dependent manner in CHO cell stably expressing hFFA2 and aequorin[1].

Reference

[1]. Lee T, et al. Identification and functional characterization of allosteric agonists for the G protein-coupled receptor FFA2. Mol Pharmacol. 2008 Dec. 74(6):1599-609.
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