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INT-777

Chemical Structure : INT-777

CAS No.: 1199796-29-6

INT-777 (S-EMCA)

Catalog No.: PC-20450Not For Human Use, Lab Use Only.

INT-777 (S-EMCA) is a potent, selective TGR5 agonist with EC50 of 0.82 uM.

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Purity & Documentation Purity: >98% (HPLC) Select Batch:

Biological Activity

INT-777 (S-EMCA) is a potent, selective TGR5 agonist with EC50 of 0.82 uM.
INT-777 (3 μM) increases ATP production in the human enteroendocrine cell line NCI-H716 in a cAMP-dependent manner.
INT-777 induces GLP-1 release in enteroendocrine cells.
INT-777 (30 mg/kg, oral) stimulates the secretion of glucagon-like peptide 1 (GLP-1) in mice after a glucose challenge.
INT-777 increases energy expenditure and reduces hepatic steatosis and adiposity in mice subjected to diet-induced obesity.
INT-777 also stimulates insulin secretion in pancreatic β-cells, reduces inflammation and inhibits atherosclerosis in mice.

Physicochemical Properties

M.Wt 450.66
Formula C27H46O5
Appearance Solid
CAS No.
Storage
Solide Powder
-20°C 12 Months; 4°C 6 Months
In Solvent
-80°C 6 Months; -20°C 6 Months
Shipping
Solubility

10 mM in DMSO

Chemical Name/SMILES

(2S,4R)-4-((3R,5S,6R,7R,8R,9S,10S,12S,13R,14S,17R)-6-ethyl-3,7,12-trihydroxy-10,13-dimethylhexadecahydro-1H-cyclopenta[a]phenanthren-17-yl)-2-methylpentanoic acid

References

1. Pellicciari R, et al. J Med Chem. 2009 Dec 24;52(24):7958-61.

2. Pruzanski M, et al. Cell Metab. 2009 Sep;10(3):167-77.

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