| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| 25mg |
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| 50mg |
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| 100mg |
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| 250mg |
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Purity: ≥98%
Fexaramine is a novel, potent, selective small molecule agonist of farnesoid X receptor (FXR) agonist with an EC50 of 25 nM and with 100-fold increased affinity relative to natural compounds. It displays no activity at hRXRα, hPPARα, hPPARγ, hPPARδ, mPXR, hPXR, hLXRα, hTRβ, hRARβ, mCAR, mERRγ and hVDR receptors. FXR is a bile acid-activated nuclear receptor that controls bile-acid synthesis, conjugation and transport, as well as lipid metabolism through actions in the liver and intestine.
| ln Vitro |
Fexaramine (5, 25, and 50 μM) was used to treat bile acids to HuTu -80 cells for a duration of 24 hours. Assay values of the small heterodimer fraction (SHP) are increased by 2.1 times when fexaramine (50 μM) is added. Endogenous protein levels were dramatically decreased (33% drop in 50 μM Fexaramine) when cells were treated with varying doses of Fexaramine. Treatment with fexaramine nonetheless markedly reduced secretin promoter activity by 32% [1].
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| ln Vivo |
Significant metabolic profiles were produced in DIO mice treated with fexaramine, including decreased inflammation, enhanced insulin adiposity, decreased weight gain, and browning of the white adipose tissue [3].
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| References |
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| Additional Infomation |
Fexaramine is a member of biphenyls.
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| Molecular Formula |
C32H36N2O3
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|---|---|
| Molecular Weight |
496.6398
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| Exact Mass |
496.273
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| CAS # |
574013-66-4
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| PubChem CID |
5326713
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| Appearance |
Light yellow to yellow solid powder
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| Density |
1.158g/cm3
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| Boiling Point |
677.7ºC at 760 mmHg
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| Flash Point |
363.7ºC
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| Index of Refraction |
1.626
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| LogP |
6.719
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| Hydrogen Bond Donor Count |
0
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| Hydrogen Bond Acceptor Count |
4
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| Rotatable Bond Count |
9
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| Heavy Atom Count |
37
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| Complexity |
743
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| Defined Atom Stereocenter Count |
0
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| SMILES |
CN(C)C1=CC=C(C=C1)C2=CC=C(C=C2)CN(C3=CC=CC(=C3)/C=C/C(=O)OC)C(=O)C4CCCCC4
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| InChi Key |
VLQTUNDJHLEFEQ-KGENOOAVSA-N
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| InChi Code |
InChI=1S/C32H36N2O3/c1-33(2)29-19-17-27(18-20-29)26-15-12-25(13-16-26)23-34(32(36)28-9-5-4-6-10-28)30-11-7-8-24(22-30)14-21-31(35)37-3/h7-8,11-22,28H,4-6,9-10,23H2,1-3H3/b21-14+
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| Chemical Name |
methyl (E)-3-(3-(N-((4'-(dimethylamino)-[1,1'-biphenyl]-4-yl)methyl)cyclohexanecarboxamido)phenyl)acrylate
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO : ~50 mg/mL (~100.68 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: 2.75 mg/mL (5.54 mM) in 5% DMSO + 40% PEG300 + 5% Tween80 + 50% Saline (add these co-solvents sequentially from left to right, and one by one), suspension solution; with sonication.
Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.5 mg/mL (5.03 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.5 mg/mL (5.03 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.0135 mL | 10.0677 mL | 20.1353 mL | |
| 5 mM | 0.4027 mL | 2.0135 mL | 4.0271 mL | |
| 10 mM | 0.2014 mL | 1.0068 mL | 2.0135 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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