INT-777

INT-777 is a potent TGR5 agonist with an EC50 of 0.82 μM[1].

Product Specifications

CAS Number

[1199796-29-6]

Product Name Alternative

S-EMCA

UNSPSC

12352211

Target

G protein-coupled Bile Acid Receptor 1

Type

Reference compound

Related Pathways

GPCR/G Protein

Field of Research

Endocrinology

Assay Protocol

https://www.medchemexpress.com/INT-777.html

Concentration

10mM

Purity

99.80

Solubility

DMSO : 100 mg/mL (ultrasonic) |Ethanol : ≥ 50 mg/mL

Smiles

O[C@@H]1CC[C@@]2(C)[C@@]([C@@H](CC)[C@@H](O)[C@]3([H])[C@]2([H])C[C@H](O)[C@@]4(C)[C@@]3([H])CC[C@@H]4[C@H](C)C[C@H](C)C(O)=O)([H])C1

Molecular Formula

C27H46O5

Molecular Weight

450.65

References & Citations

[1]Pellicciari R, et al. Discovery of 6alpha-ethyl-23 (S) -methylcholic acid (S-EMCA, INT-777) as a potent and selective agonist for the TGR5 receptor, a novel target for diabesity. J Med Chem. 2009 Dec 24;52 (24) :7958-61.|[2]Thomas C, et al. TGR5-mediated bile acid sensing controls glucose homeostasis. Cell Metab. 2009 Sep;10 (3) :167-77.|[3]Duboc H, et al.Reduction of epithelial secretion in male rat distal colonic mucosa by bile acid receptor TGR5 agonist, INT-777: role of submucosal neurons. Neurogastroenterol Motil. 2016 Jun 3. doi: 10.1111/nmo.|[4]Baiqiang Li, et al. INT-777, a bile acid receptor agonist, extenuates pancreatic acinar cells necrosis in a mouse model of acute pancreatitis. Biochem Biophys Res Commun. 2018 Sep 3;503 (1) :38-44.