Keyword:Dapiglutide,2296814-85-0,dapiglutide peptide
Research Progress on Metabolism and Gut Health under the Synergistic Effect of GLP-1R/GLP-2R Dual Targets
In the field of metabolic and gut health research, the development of novel compounds has always been key to breaking through the bottlenecks in disease intervention. Dapiglutide (CAS No.: 2296814-85-0, also known as ZP7570), as a long-acting dual agonist of glucagon-like peptide-1 receptor (GLP-1R)/glucagon-like peptide-2 receptor (GLP-2R), has become a research hotspot in recent years due to its unique dual-target mechanism of action, and related literature studies are gradually unlocking its potential application value.
Core Advantage: Synergistic Activation Characteristics of GLP-1R/GLP-2R Dual Receptors
Compared to single-target drugs, the core advantage of Dapiglutide lies in the synergistic activation of GLP-1R and GLP-2R. In vitro studies showed that in HEK293 cell experiments, its half-maximal effective concentration (EC₅₀) for GLP-1R was 190 pm, and its EC₅₀ for GLP-2R was 210 pm, exhibiting excellent receptor binding activity and selectivity. This characteristic allows it to exert both the metabolic regulatory effect of GLP-1R agonists and the intestinal protective function of GLP-2R agonists, forming unique scientific research value.
Animal Experiments Validate: Metabolic and Intestinal Protective Efficacy Highlighted
Animal experiments further validated its efficacy. In a mouse short bowel syndrome model constructed by 40% ileocecal resection, subcutaneous injection of Dapiglutide at a dose of 6-250 nmol/kg once daily for 3 consecutive days significantly improved oral glucose tolerance, shortened intestinal transit time, and promoted intestinal growth while reducing fecal water loss. In an obese mouse model, daily injection of 100 nmol/kg for 4 consecutive weeks resulted in weight loss, with more significant effects when used in combination with ZP8396.
Pharmacokinetic Characteristics and Clinical Research Progress
Pharmacokinetic studies show that after subcutaneous injection, the half-life in mice is 3.6 hours, the time to peak concentration is 4.5 hours, and the bioavailability is 71%; in rats, the half-life is 7.7 hours, the time to peak concentration is 9.0 hours, and the bioavailability is 58%. These favorable characteristics lay the foundation for clinical translation. Currently, several clinical trials, including NCT05788601 and NCT06758583, are exploring its application potential in obesity and inflammation.
Research Summary and Outlook
As a novel dual-receptor agonist, the research on Dapiglutide (2296814-85-0) has enriched the research and development ideas in the fields of metabolism and gut health, providing new candidate molecules for precise intervention in related diseases. With the deepening of clinical research, we look forward to unlocking more clinical value and empowering human health.
