INT-777 is a potent agonist of TGR5 (EC50: 0.82 μM).

INT-777 has remarkable in vivo activity[1]. INT-777 effect on basal secretion is reduced in neuron-free and TTX-treated mucosal-submucosal preparations[3]. INT-777 (3 μM) enhances 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 (1 μM/min/kg, p.o.) has an effective choleretic effect and 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.) enhances energy expenditure and decreases hepatic steatosis and obesity upon high-fat feeding in TGR5-Tg mice[2].

1199796-29-6

C27H46O5

450.65

S-EMCA

DMSO:31 mg/mL (68.79 mM)
Ethanol:50 mg/mL (110.95 mM)
Powder: -20°C for 3 years
In solvent: -80°C for 2 years