Fexaramine
Chemical Name: 3-[3-[(Cyclohexylcarbonyl)-[[4'-(dimethylamino)-[1,1'-biphenyl]-4-yl]methyl]amino]phenyl]-2-propenoic acid methyl ester
Purity: ≥97%
Biological Activity
Fexaramine is a potent, selective farnesoid X receptor agonist (EC50 = 25 nM). Displays no activity at hRXRα, hPPARα, hPPARγ, hPPARδ, mPXR, hPXR, hLXRα, hTRβ, hRARβ, mCAR, mERRγ and hVDR receptors.Technical Data
The technical data provided above is for guidance only.
For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.
Background References
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Positive regulation of osteogenesis by bile acid through FXR.
Cho S, An J, Park H, Yang J, Choi H, Kim S, Park Y, Kim S, Yim M, Baek W, Kim J, Shin C
J Bone Miner Res, 2013;28(10):2109-21. -
Discovery and optimization of non-steroidal FXR agonists from natural product-like libraries.
Nicolaou et al.
Org.Biomol.Chem., 2003;1:908 -
A chemical, genetic, and structural analysis of the nuclear bile acid receptor FXR.
Downes et al.
Mol.Cell, 2003;11:1079 -
Back door modulation of the farnesoid X receptor: design, synthesis, and biological evaluation of a series of side chain modified chenodeoxycholic acid derivatives.
Pellicciari et al.
J.Med.Chem., 2006;49:4208
Product Datasheets
Citation for Fexaramine
The citations listed below are publications that use Tocris products. Selected citations for Fexaramine include:
1 Citation: Showing 1 - 1
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Modulators of hepatic lipoprotein metabolism identified in a search for small-molecule inducers of tribbles pseudokinase 1 expression.
Authors: Nagiec Et al.
J Endocrinol 2015;10:e0120295
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