INT-777

1199796-29-6

C27H46O5

DMSO : >= 31 mg/mL (68.79 mM); Ethanol : >= 50 mg/mL (110.95 mM)

GPCR/G Protein

INT-777 is a potent TGR5 agonist with an EC₅₀ of 0.82 uM. IC50 & Target: EC50: 0.82 uM (TGR5)^[1] In Vitro: INT-777 is a novel potent and selective TGR5 agonist with remarkable in vivo activity^[1]. INT-777 (3 uM) increases ATP production in the human enteroendocrine cell line NCI-H716 in a cAMP-dependent manner^[2]. INT-777 (10 uM) 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 uM/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, and improves insulin sensitivity, in TGR5-Tg mice^[2].