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Submit ReviewFexaramine
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)
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 |
| InChI Key | VLQTUNDJHLEFEQ-KGENOOAVSA-N |
| 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 | |
|---|---|---|---|
| Solubility | |||
| 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.
| 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
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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