产品
编 号：F754299
分子式：C29H27N3O6
分子量：513.54
分子式：C29H27N3O6
分子量：513.54
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CAS No: 2643391-08-4
产品详情
生物活性：
TGR5 Receptor Agonist 3 (Compound 19) is a soft-agent G-protein-coupled bile acid receptor 1 (GPBAR1, TGR5) agonist with reduced gallbladder-filling effects (favorable gallbladder safety), with EC50s of 16.4 and 209 nM for hTGR5 and mTGR5, respectively.
体内研究：
TGR5 Receptor Agonist 3 (compound 19) has good targeting and can effectively activate TGR5, thus promoting the secretion of GLP-1 in plasma and regulating the homeostasis of glucose metabolism in male ICR mice.TGR5 Receptor Agonist 3 (compound 19) can be rapidly absorbed and metabolized in male ICR mice, and has a good safety profile.TGR5 Receptor Agonist 3 (compound 19) (oral gavage; 50 mg/kg; one hour) can be gavaged into overnight-fasted male ICR mice for one hour with a Cmaxvalue of 0.003 μg/mL .TGR5 Receptor Agonist 3 (compound 19) can reduce gallbladder-filling and safety in vivo.
体外研究：
TGR5 Receptor Agonist 3 (compound 19) (10-50μM, 2 hours) activates TGR5 in fetal rat intestinal cells (FRIC) and NCI-H716 cells to promote GLP-1 secretion in a dose-dependent manner.
TGR5 Receptor Agonist 3 (Compound 19) is a soft-agent G-protein-coupled bile acid receptor 1 (GPBAR1, TGR5) agonist with reduced gallbladder-filling effects (favorable gallbladder safety), with EC50s of 16.4 and 209 nM for hTGR5 and mTGR5, respectively.
体内研究：
TGR5 Receptor Agonist 3 (compound 19) has good targeting and can effectively activate TGR5, thus promoting the secretion of GLP-1 in plasma and regulating the homeostasis of glucose metabolism in male ICR mice.TGR5 Receptor Agonist 3 (compound 19) can be rapidly absorbed and metabolized in male ICR mice, and has a good safety profile.TGR5 Receptor Agonist 3 (compound 19) (oral gavage; 50 mg/kg; one hour) can be gavaged into overnight-fasted male ICR mice for one hour with a Cmaxvalue of 0.003 μg/mL .TGR5 Receptor Agonist 3 (compound 19) can reduce gallbladder-filling and safety in vivo.
体外研究：
TGR5 Receptor Agonist 3 (compound 19) (10-50μM, 2 hours) activates TGR5 in fetal rat intestinal cells (FRIC) and NCI-H716 cells to promote GLP-1 secretion in a dose-dependent manner.
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