INT-777 R-enantiomer

Names

[ CAS No. ]:
1198786-98-9

[ Name ]:
INT-777 R-enantiomer

[Synonym ]:
(2R,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
INT-777 (R-enantiomer)

Biological Activity

[Description]:

INT-777 (R-enantiomer) is the R-enantiomer of INT-777, with EC50 of 4.79 μM for TGR5, and less potent than INT-777.

[Related Catalog]:

Signaling Pathways >> GPCR/G Protein >> GPCR19
Research Areas >> Others

[In Vivo]

INT-777 (R-enantiomer) is more choleretic than CA (4), but less than INT-777[1].

[References]

[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.


[Related Small Molecules]

INT-777 | INT-767 | Deoxycholic acid | BAR501 | TGR5 | SB756050 | BAR502 | Hyodeoxycholic acid

Chemical & Physical Properties

[ Density]:
1.1±0.1 g/cm3

[ Boiling Point ]:
602.8±55.0 °C at 760 mmHg

[ Molecular Formula ]:
C27H46O5

[ Molecular Weight ]:
450.651

[ Flash Point ]:
332.4±28.0 °C

[ Exact Mass ]:
450.334534

[ LogP ]:
3.99

[ Vapour Pressure ]:
0.0±3.9 mmHg at 25°C

[ Index of Refraction ]:
1.539

[ Storage condition ]:
2-8℃

Related Compounds