INT-767

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

INT-767 是一种有效的、选择性的法尼醇 X 受体 (FXR) 和 TGR5 双重激动剂，EC50 分别为 30 和 630 nM。

INT-767 is a potent, selective, dual farnesoid X receptor (FXR) and TGR5 agonist with EC50 of 30 and 630 nM, respectively; fails to activate 15 other nuclear receptors involved in metabolic pathways, and does not inhibit cytochrome P450 enzymes; induces FXR-dependent lipid uptake by adipocytes and promotes TGR5-dependent glucagon-like peptide-1 (GLP-1) secretion by enteroendocrine cells; markedly decreases cholesterol and triglyceride levels in diabetic db/db mice.Fibrosis Phase 1 Clinical.

INT-767 does not show cytotoxic effects in HepG2 cells, does not inhibit cytochrome P450 enzymes, is highly stable to phase I and II enzymatic modifications, and does not inhibit the human ether-a-go-go-related gene potassium channel.

INT-767 (10-20 mg/kg; i.p.; daily for 2 weeks) decreases plasma total cholesterol and triglyceride levels in db/m and db/db mice . Animal Model:Male 8-week old C57BKS/J db/db mice, control nondiabetic db/m mice Dosage:10, 20 mg/kg Administration:Intraperitoneal injection; daily for 2 weeks Result:Decreased plasma total cholesterol and triglyceride levels.

INT767

Metabolic Enzyme/Protease

FXR

FXR

Other Indications

Fibrosis

1000403-03-1

494.6601

C25H43NaO6S

>98% (HPLC)

DMSO: ≥ 205.5 mg/mL

O[C@@H]1CC[C@@]2(C)[C@@]([C@@H](CC)[C@@H](O)[C@]3([H])[C@]2([H])CC[C@@]4(C)[C@@]3([H])CC[C@@]4([C@H](C)CCOS(=O)([O-])=O)[H])([H])C1.[Na+]

24-Norcholane-3,7,23-triol, 6-ethyl-, 23-(hydrogen sulfate), sodium salt (1:1), (3α,5β,6α,7α)-

(-20℃)

With Ice Pack

≥ 2 years