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Fexaramine

Names

[ CAS No. ]:
574013-66-4

[ Name ]:
Fexaramine

[Synonym ]:
Fexaramine

Biological Activity

[Description]:

Fexaramine is a small molecule farnesoid X receptor (FXR) agonist with 100-fold increased affinity relative to natural compounds. IC50 value:Target:in vitro: In vitro treatment of CDCA or fexaramine elevated the SHP transcript level and occupancy on secretin promoter [1]. Fexaramine significantly enhanced osteoblastic differentiation through the upregulation of Runx2 and enhanced extracellular signal-regulated kinase (ERK) and β-catenin signaling [2]. By mimicking this tissue-selective effect, the gut-restricted FXR agonist fexaramine (Fex) robustly induces enteric fibroblast growth factor 15 (FGF15), leading to alterations in BA composition, but does so without activating FXR target genes in the liver [3].

[Related Catalog]:

Signaling Pathways >> Metabolic Enzyme/Protease >> FXR
Research Areas >> Others

[References]

[1]. Lam IP, et al. Bile acids inhibit duodenal secretin expression via orphan nuclear receptor small heterodimer partner (SHP). Am J Physiol Gastrointest Liver Physiol. 2009 Jul;297(1):G90-7.

[2]. Cho SW, et al. Positive regulation of osteogenesis by bile acid through FXR. J Bone Miner Res. 2013 Oct;28(10):2109-21.

[3]. Fang S, et al. Intestinal FXR agonism promotes adipose tissue browning and reduces obesity and insulin resistance. Nat Med. 2015 Feb;21(2):159-65.


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Chemical & Physical Properties

[ Density]:
1.158g/cm3

[ Boiling Point ]:
677.7ºC at 760 mmHg

[ Molecular Formula ]:
C32H36N2O3

[ Molecular Weight ]:
496.64000

[ Flash Point ]:
363.7ºC

[ Exact Mass ]:
496.27300

[ PSA ]:
49.85000

[ LogP ]:
6.71930

[ Appearance of Characters ]:
yellow solid

[ Index of Refraction ]:
1.626

[ Storage condition ]:
-20℃

Safety Information

[ Symbol ]:

GHS07

[ Signal Word ]:
Warning

[ Hazard Statements ]:
H302-H413

[ Precautionary Statements ]:
P301 + P312 + P330

[ RIDADR ]:
NONH for all modes of transport


Related Compounds