Network Version
INT-777 Data Sheet
| Product Name: | INT-777 |
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|---|---|---|
| CAS No.: | 1199796-29-6 | |
| Cat. No.: | HY-15677 | |
| MWt: | 450.65 | |
| Formula: | C27H46O5 | |
| Purity : | >98% | |
| Solubility: | DMSO : ≥ 31 mg/mL (68.79 mM); Ethanol : ≥ 50 mg/mL (110.95 mM) | |
| Mechanisms: | Target: Endocrinology | |
| Biological Activity: | ||
| INT-777 is a potent TGR5 agonist with an EC50 of 0.82 μM. IC50 & Target: EC50: 0.82 μM (TGR5)[1] In Vitro: INT-777 is a novel potent and selective TGR5 agonist with remarkable in vivo activity[1]. INT-777 (3 μM) increases ATP production in the human enteroendocrine cell line NCI-H716 in a cAMP-dependent manner[2]. INT-777 (10 μM) lowers Isc and increases TEER when added on the serosal side of seromuscular stripped distal colon segments. INT-777 effect on basal secretion is reduced in neuron-free and TTX-treated mucosal-submucosal preparations[3]. 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[1]. INT-777 (30 mg/kg/day, p.o.) increases energy expenditure and reduces hepatic steatosis and obesity upon high fat feeding in TGR5-Tg mice[2]. | ||
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