934613-63-5Relevant academic research and scientific papers
Discovery of N-Aryl-2-acylindole human glucagon receptor antagonists
Sinz, Christopher,Bittner, Amy,Brady, Ed,Candelore, Mari,Dallas-Yang, Qing,Ding, Victor,Jiang, Guoqiang,Lin, Zhen,Qureshi, Sajjad,Salituro, Gino,Saperstein, Richard,Shang, Jackie,Szalkowski, Deborah,Tota, Laurie,Vincent, Stella,Wright, Michael,Xu, Shiyao,Yang, Xiaodong,Zhang, Bei,Tata, James,Kim, Ronald,Parmee, Emma R.
, p. 7124 - 7130 (2012/01/13)
A novel class of N-aryl-2-acylindole human glucagon receptor (hGCGR) antagonists is reported. These compounds demonstrate good pharmacokinetic profiles in multiple preclinical species. One compound from this series, indole 33, is orally active in a transgenic murine pharmacodynamic model. Furthermore, a 1 mg/kg oral dose of indole 33 lowers ambient glucose levels in an ob/ob/hGCGR transgenic murine diabetes model. This compound was deemed suitable for preclinical safety studies and was found to be well tolerated in an 8-day experimental rodent tolerability study. The combination of preclinical efficacy and safety observed with compound 33 highlights the potential of this class as a treatment for type 2 diabetes.
