AZD7687

AZD7687 is a potent, selective, reversible and orally active diacylglycerol acyltransferase 1 (DGAT1) inhibitor with an IC₅₀ of 80 nM for human DGAT1. AZD7687 can be used for type 2 diabetes mellitus and obesity research^[1][2]. In Vitro:In an in vitro recombinant mouse, dog, and human DGAT1 enzyme assay, AZD7687 has an IC50 of approximately 100 nM, 60 nM, and 80 nM, respectively. AZD7687 (compound 30) shows inhibition of acyl-CoA:cholesterol acetyltransferase (79% at 10 μM), fatty acid amide hydrolase (IC₅₀ = 3.7 μM), muscarinic M2 receptor (IC₅₀ = 80.5 μM), and phosphodiesterase PDE10A1 (IC₅₀ = 5.5 μM). No activity against human DGAT2 is detected^[1][2]. In Vivo:Prolonged pharmacological inhibition of DGAT1 with AZD7687 in mice results in the same skin phenotype, including sebaceous gland atrophy and alopecia, as seen in the skin of DGAT1^-/- mice. AZD7687-mediated effects on the skin were dose- and time-dependent and reversible^[3].