6,6-Dimethyl-3-(4-methylbenzoyl)-4,5,6,7-tetrahydro-1-benzothiophen-2-amine is a glucagon-like peptide 1 receptor (GLP-1R) positive allosteric modulator (PAM).1 It increases GLP-1-induced cAMP production by 268.35% in a reporter assay using HEK293 cells expressing human GLP-1R. 6,6-Dimethyl-3-(4-methylbenzoyl)-4,5,6,7-tetrahydro-1-benzothiophen-2-amine (5 ?M) induces insulin secretion in glucose-stimulated GLP-1 (7-36)-induced INS-1 832/13 cells. It decreases blood glucose levels in a glucose tolerance test in fasted mice when administered at doses of 10 or 30 mg/kg.
References:
[1]. Campbell, J.A., Do, P., Li, Z., et al.Synthesis and biological studies of 2-aminothiophene derivatives as positive allosteric modulators of glucagon-like peptide 1 receptorBioorg. Med. Chem.111117864(2024).