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Description: Potent, selective farnesoid X receptor (FXR) agonist
Chemical Name: 3-[3-[(Cyclohexylcarbonyl)-[[4'-(dimethylamino)-[1,1'-biphenyl]-4-yl]methyl]amino]phenyl]-2-propenoic acid methyl ester
Purity: ≥97% (HPLC)
Citations (1)

Biological Activity for Fexaramine

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.

Compound Libraries for Fexaramine

Fexaramine is also offered as part of the Tocriscreen 2.0 Max. Find out more about compound libraries available from Tocris.

Technical Data for Fexaramine

M. Wt 496.64
Formula C32H36N2O3
Storage Desiccate at +4°C
Purity ≥97% (HPLC)
CAS Number 574013-66-4
PubChem ID 5326713
Smiles O=C(C3CCCCC3)N(CC2=CC=C(C4=CC=C(N(C)C)C=C4)C=C2)C1=CC(/C=C/C(OC)=O)=CC=C1

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.

Solubility Data for Fexaramine

Solvent Max Conc. mg/mL Max Conc. mM
DMSO 49.66 100

Preparing Stock Solutions for Fexaramine

The following data is based on the product molecular weight 496.64. Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Select a batch to recalculate based on the batch molecular weight:
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 2.01 mL 10.07 mL 20.14 mL
5 mM 0.4 mL 2.01 mL 4.03 mL
10 mM 0.2 mL 1.01 mL 2.01 mL
50 mM 0.04 mL 0.2 mL 0.4 mL

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Product Datasheets for Fexaramine

Certificate of Analysis / Product Datasheet
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References for Fexaramine

References are publications that support the biological activity of the product.

Nicolaou et al (2003) Discovery and optimization of non-steroidal FXR agonists from natural product-like libraries. Org.Biomol.Chem. 1 908 PMID: 12929628

Downes et al (2003) A chemical, genetic, and structural analysis of the nuclear bile acid receptor FXR. Mol.Cell 11 1079 PMID: 12718892

Pellicciari et al (2006) Back door modulation of the farnesoid X receptor: design, synthesis, and biological evaluation of a series of side chain modified chenodeoxycholic acid derivatives. J.Med.Chem. 49 4208 PMID: 16821780

If you know of a relevant reference for Fexaramine, please let us know.

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Keywords: Fexaramine, Fexaramine supplier, Potent, selective, farnesoid, X, receptor, FXR, agonists, Receptors, Liver, Farnesoid, LXR-like, 2563, Tocris Bioscience

1 Citation for Fexaramine

Citations are publications that use Tocris products. Selected citations for Fexaramine include:

Nagiec et al (2015) Modulators of hepatic lipoprotein metabolism identified in a search for small-molecule inducers of tribbles pseudokinase 1 expression. J Endocrinol 10 e0120295 PMID: 25811180

Do you know of a great paper that uses Fexaramine from Tocris? Please let us know.

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