期刊
BIOORGANIC & MEDICINAL CHEMISTRY
卷 35, 期 -, 页码 -出版社
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmc.2021.116071
关键词
GPR119 agonist; Thiazolidinediones (TZDs); Type 2 diabetes mellitus (T2DM); Insulin sensitizers
This research aims at finding an effective oral GPR 119 agonist, which showed good results in cell-based assays and animal models without displaying toxicity.
The ever-growing prevalence of Type-2 diabetes in the world has an urgent need for multiple orally effective agents that can regulate glucose homeostasis. G-Protein coupled receptor 119 (GPR 119) agonists have demonstrated the glucose-dependent insulin secretion and showed beneficial effects on glycemic control in humans and/or relevant animal models. Herein, we describe our efforts towards identification of a potent and oral GPR 119 agonist 13c (ZY-G19), which showed in vitro potency in the cell-based assay and in vivo efficacy without exerting any significant signs of toxicity in relevant animal models.
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