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Purity: ≥98%
Choline fenofibrate (formerly also known as ABT-335 or choline salt of fenofibric acid) is a novel, synthetic phenoxy-isobutyric acid derivate with antihyperlipidemic activity that acts as an PPARα agonist. It was being developed clinically as a rosuvastatin combination therapy to treat dyslipidemia. This lipid-regulating substance can be taken orally as delayed-release capsules. The activation of peroxisome proliferator activated receptor α (PPARα) in vitro in human hepatocyte cultures and in vivo in transgenic mice explains the lipid-modifying effects of fenofibric acid observed in clinical practice. Fenofibric acid works by activating lipoprotein lipase and decreasing the production of Apo CIII, an inhibitor of lipoprotein lipase activity, to increase lipolysis and the removal of triglyceride-rich particles from plasma. Additionally, increased synthesis of HDL-C, Apo AI, and AII is induced by PPARα activation.
| Targets |
PPAR
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|---|---|
| ln Vitro |
WAY-316606 inhibits spontaneous HF regression (catagen) ex vivo and increases hair shaft production and keratin expression in the hair shaft. In mammalian skin cell populations, WAY-316606 efficiently increases β-catenin activity in human hair pre-cortex keratinocytes and DP fibroblasts ex vivo.
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| ln Vivo |
Choline Fenofibrate, when administered orally (rat 4 mg/kg), shows excellent absolute oral bioavailability (rat 93.4%) and Cmax (rat 7944.2 ng/mL)[1].
Choline Fenofibrate demonstrates a terminal elimination half-life of 5.4 hours in rats after an IV injection of 4 mg/kg[1]. |
| Animal Protocol |
Male Sprague-Dawley (SD) rats (200-250g)[1]
4 mg/kg (Pharmacokinetic Analysis) Intravenous injection and oral administration |
| References |
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| Molecular Formula |
C22H28CLNO5
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| Molecular Weight |
421.92
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| Exact Mass |
421.1656007
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| Elemental Analysis |
C, 62.63; H, 6.69; Cl, 8.40; N, 3.32; O, 18.96
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| CAS # |
856676-23-8
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| Related CAS # |
Fenofibric acid;42017-89-0;Choline chloride;67-48-1
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| Appearance |
White to light yellow solid powder.
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| SMILES |
CC(C)(C(=O)[O-])OC1=CC=C(C=C1)C(=O)C2=CC=C(C=C2)Cl.C[N+](C)(C)CCO
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| InChi Key |
JWAZHODZSADEHB-UHFFFAOYSA-M
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| InChi Code |
InChI=1S/C17H15ClO4.C5H14NO/c1-17(2,16(20)21)22-14-9-5-12(6-10-14)15(19)11-3-7-13(18)8-4-11;1-6(2,3)4-5-7/h3-10H,1-2H3,(H,20,21);7H,4-5H2,1-3H3/q;+1/p-1
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| Chemical Name |
2-[4-(4-chlorobenzoyl)phenoxy]-2-methylpropanoate;2-hydroxyethyl(trimethyl)azanium
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| Synonyms |
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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 |
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| 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) |
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (5.93 mM) (saturation unknown) in 10% EtOH + 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 EtOH 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. Solubility in Formulation 2: ≥ 2.5 mg/mL (5.93 mM) (saturation unknown) in 10% EtOH + 90% (20% SBE-β-CD in 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 EtOH stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.5 mg/mL (5.93 mM) (saturation unknown) in 10% EtOH + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. Solubility in Formulation 4: ≥ 2 mg/mL (4.74 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 20.0 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. Solubility in Formulation 5: ≥ 2 mg/mL (4.74 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in 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 20.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.3701 mL | 11.8506 mL | 23.7012 mL | |
| 5 mM | 0.4740 mL | 2.3701 mL | 4.7402 mL | |
| 10 mM | 0.2370 mL | 1.1851 mL | 2.3701 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.
| NCT Number | Recruitment | interventions | Conditions | Sponsor/Collaborators | Start Date | Phases |
| NCT05365425 | Recruiting | Drug: Choline fenofibrate Drug: Policosanol |
Dyslipidemia Atherosclerosis |
Seoul National University Bundang Hospital |
June 1, 2023 | Phase 4 |
| NCT00673881 | Completed | Drug: choline fenofibrate | Dyslipidemia | Radiant Research | March 2008 | Phase 1 Phase 2 |
| NCT00683176 | Completed | Drug: Choline Fenofibrate Drug: Placebo |
Diabetic Macular Edema | Abbott Products | September 2008 | Phase 2 |
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