The aims of this study were to investigate a GCGR-biased co-agonist as treatment for hepatic steatosis in mice. METHODS: Mice with diet-induced obesity (DIO) were treated with Dicretin, a GLP1/GCGR co-agonist with high potency at the GCGR, Semaglutide (GLP1R monoagonist) or food ...
(2) 胡中平等 :GLP-1R 结构和功能及小分子药物筛选研究进展 37 鼠 HbA1c 含量到正常水平.由于它们缺乏类药分子 所具有的结构特征(背离了 Lipinsky 和 Veber 规律), Boc5 只是作为一种有用的概念性分子,并且有关该 分子结合受体的机理可能同 GLP-1 类似[52].2007 年发现另外一种非肽类激动剂,compound2(...
in body weight (P<0.001), blood glucose levels in OGTT (P<0.001), HbA1c(P<0.05) and improved insulin resistance (P<0.01). Notably, it increased peripheral adipocyte density and resolved hepatic steatosis. The efficacy of SAL0112 was found to be comparable to that of Danuglipron and ...
(B) PPP1R1A mRNA levels in type 2 diabetic (n = 31) and non-diabetic (ND, n = 160) donor islets, ****p < 0.0001. (CD) Rank-Spearman correlation analysis of PPP1R1A mRNA levels with: (C) HbA1c (mmol/mol) (r = −0.43, p < 0.0001, n = 173)...
In db/db mice, BI 456906 and BI 456908 (10 and 20 nmol/kg qd) substantially lowered HbA1c (0.4-0.6%); no clear effect was observed for BI 456897 (3 and 7 nmol/kg qd). As a balanced GCGR/GLP-1R agonist with robust in vivo efficacy BI 456906 (30 nmol/kg qd) was further ...
GLP-1R agonist is independent of the hypoglycemic effect of T2DM and has protective effect on cardiovascular system. GLP-1R may regulate the polarization of macrophages toward M2, thus playing a protective role in the progression of coronary atherosclerosis. 1. Introduction Type 2 diabetes mellitus ...
However, the precise role and importance of cAMP in mediating GLP1R`s anti-inflammatory actions, at least in the heart, remains to be determined. To this end, we tested the effects of the GLP1R agonist liraglutide on lipopolysaccharide (LPS)-induced acute inflammatory injury in H9c2 cardiac ...
1874-LB: PG-102, a Bivalent GLP-1R/GLP-2R Agonist, Protects -Cell Mass and Enhances Glycemic Control in Obese db/db Mice, Showing Superiority over Semaglutide, Tirzepatide, and Retatrutidedoi:10.2337/db24-1874-LBPG-102, a first-in-class heterodimeric Fc fusion protein, simultaneously ...
(T2D) –– CT-868 administered once-daily over 26 weeks showed robust glycemic control with ~70% of patients with T2D achieving HbA1c in the non-diabetes range –– Mechanistic studies in rodent models demonstrates that G-protein biased signaling in the central nervous system leads to sustained...
1. A combination comprising an FGF21 (fibroblast growth factor 21) compound and a GLP-1R (glucagon-like peptide-1 receptor) agonist, wherein the FGF21 compound has an FGF21 activity which is the same or substantially the same as the FGF21 activity of native FGF21 and is an FGF21 varian...