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INT-777 is a novel potent and selective TGR5 agonist. INT-777 (3 μM) increases ATP production in the human enteroendocrine cell line NCI-H716 in a cAMP-dependent manner. INT-777 (10 μM) lowers Isc and increases TEER when added on the serosal side of seromuscular stripped distal colon segments.
In vivo, INT-777 (1 μM/min/kg, p.o.) has a potent choleretic effect, prevents carboxyl CoA activation and subsequent conjugation, thereby favoring its cholehepatic shunt pathway with a ductular absorption and a potent choleretic effect in HF-fed TGR5-Tg male mice. INT-777 (30 mg/kg/day, p.o.) increases energy expenditure and reduces hepatic steatosis and obesity upon high fat feeding, and improves insulin sensitivity, in TGR5-Tg mice.
| Cell Experiment | |
|---|---|
| Cell lines | Cardiomyocytes cells |
| Preparation method | To determine the effect of TGR5 on the inflammatory response, cardiomyocytes were infected with TGR5 shRNA adenoviral particles for 24 h or pretreated with 100 μM SQ22536 (cAMP inhibitor) for 3 h and then treated with 30 μM INT-777 (selective TGR5 agonist) for 3 h, followed by exposure to HG for 6 h. As shown by western blotting, pretreatment of cardiomyocytes with INT-777 inhibited HG-induced protein expression of p-IκBα, whereas the inhibitory effect of INT-777 was attenuated by TGR5 shRNA or SQ22536. |
| Concentrations | 30 μM |
| Incubation time | 3 h |
| Animal Experiment | |
|---|---|
| Animal models | C57BL/6 J Mice |
| Formulation | DMSO and Saline |
| Dosages | 0.375 μg, 0.75 μg and 1.5 μg/mouse/day |
| Administration | i.c.v |
| Molecular Weight | 450.65 |
| Formula | C27H46O5 |
| CAS Number | 1199796-29-6 |
| Form | Solid |
| Solubility (25°C) | DMSO: ≥ 25 mg/mL |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
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