INT-777,1199796-29-6

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产品名称：INT-777

产品别名：见爱必信官网

英文别名：INT-777

靶点：GPCR19

CAS：1199796-29-6

纯度：见爱必信官网

外观：见爱必信官网

保存方法：见爱必信官网

描述：INT-777 is a potent TGR5 agonist with an EC50 of 0.82 μM.

溶解性：DMSO: ≥ 31 mg/mL

体外研究：

INT-777 is a novel potent and selective TGR5 agonist with remarkable in vivo activity. 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. INT-777 effect on basal secretion is reduced in neuron-free and TTX-treated mucosal-submucosal preparations.

体内研究：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.

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