Ciprofibrate
Based on 1 Customer Validation
Ciprofibrate (Win35833) is a potent peroxisome proliferator and increases the phosphorylation level of the PPARalpha. Ciprofibrate acts as an orally active hypolipidaemic agent and can be used for the research of primary hyperlipidaemias.
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- Purity: 99.93%
- CAS No.: 52214-84-3
- 화학식: C13H14Cl2O3
- 분자량:289.15
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보관:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
Biological Activity
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PPARα |
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| HepG2 | EC50 |
0.9 μM
Compound: Ciprofibrate
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Transactivation of GAL4-fused PPARalpha LBD expressed in HepG2 cells after 20 hrs by luminescence assay
Transactivation of GAL4-fused PPARalpha LBD expressed in HepG2 cells after 20 hrs by luminescence assay
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[PMID: 22381047] |
| HepG2 | EC50 |
0.9 μM
Compound: CPF
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Transactivation of GAL4-fused PPARalpha ligand binding domain transfected in human HepG2 cells after 20 hrs by luciferase reporter gene assay
Transactivation of GAL4-fused PPARalpha ligand binding domain transfected in human HepG2 cells after 20 hrs by luciferase reporter gene assay
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[PMID: 23031596] |
| Sf21 | IC50 |
189.9 μM
Compound: Ciprofibrate
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Inhibition of Sprague-Dawley rat Bsep expressed in plasma membrane vesicles of Sf21 cells assessed as inhibition of ATP-dependent [3H]taurocholate uptake
Inhibition of Sprague-Dawley rat Bsep expressed in plasma membrane vesicles of Sf21 cells assessed as inhibition of ATP-dependent [3H]taurocholate uptake
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[PMID: 21965623] |
| Sf21 | IC50 |
572.7 μM
Compound: Ciprofibrate
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Inhibition of human BSEP expressed in plasma membrane vesicles of Sf21 cells assessed as inhibition of ATP-dependent [3H]taurocholate uptake
Inhibition of human BSEP expressed in plasma membrane vesicles of Sf21 cells assessed as inhibition of ATP-dependent [3H]taurocholate uptake
|
[PMID: 21965623] |
Ciprofibrate (500 μM; 4 hours) increases the PPARa phosphorylation level in rat Fao cells[1].In a LucLite assay, Ciprofibrate (10-100μM; 24 hours) induces PPARR activation by existing increased LUC activities in the rat liver H4IIEC3 cells transfected with PPRE-AB LUC reporter gene plasmid[2].Ciprofibrate (10-100 μM; 24 hours) is not cytotoxic for HepG2 cells, and the cell viability is 99.7%[3].Ciprofibrate (100 μM; 24 hours) also abolishes FFAs mixture-induced lipid deposition and decreases FFAs mixture-increased TG contents?in HepG2 cells[3].Ciprofibrate (100 μM; 24 hours) almost entirely eliminates the FFAs mixture-induced inflammatory cytokines overproduction, including MCP-1, TNF-α, and IL-6 in HepG2 cells[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:C57BL/6 mice (six-week-old males)[3]
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Dosage:10 mg/kg
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Administration:Oral administration; 10 mg/kg/day; 3 days
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Result:Decreased MCD diet-resulted hepatic steatosis and hepatic necro-inflammation in mice.
Chemical Information
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CAS No. 52214-84-3
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Appearance Solid
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분자량 289.15
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화학식 C13H14Cl2O3
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Color White to off-white
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SMILES
CC(C)(OC1=CC=C(C2C(Cl)(Cl)C2)C=C1)C(O)=O
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Synonyms
Win35833
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선적
Room temperature in continental US; may vary elsewhere.
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보관
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
용액&용해도
DMSO : ≥ 100 mg/mL (345.84 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
* "≥" means soluble, but saturation unknown.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (8.65 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.5 mg/mL (8.65 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
순도&문서
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Data Sheet (273 KB)
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SDS (418 KB)
- English - EN (418 KB)
- Français - FR (418 KB)
- Deutsch - DE (418 KB)
- Norwegian - NO (418 KB)
- Español - ES (418 KB)
- Swedish - SV (418 KB)
- Italian - IT (418 KB)
- Korean - KR (418 KB)
- Portuguese - PT (418 KB)
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Handling Instructions (2659 KB)
References
[1]. Passilly, P., et al., Phosphorylation of peroxisome proliferator-activated receptor alpha in rat Fao cells and stimulation by ciprofibrate. Biochem Pharmacol, 1999. 58(6): p. 1001-8. [Content Brief]
[2]. Agnes M Rimando, et al. Pterostilbene, a new agonist for the peroxisome proliferator-activated receptor alpha-isoform, lowers plasma lipoproteins and cholesterol in hypercholesterolemic hamsters. J Agric Food Chem. 2005 May 4;53(9):3403-7. [Content Brief]
[3]. Thing-Fong Tzeng, et al. 6-gingerol protects against nutritional steatohepatitis by regulating key genes related to inflammation and lipid metabolism. Nutrients. 2015 Feb 4;7(2):999-1020. [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 3.4584 mL | 17.2921 mL | 34.5841 mL | 86.4603 mL |
| 5 mM | 0.6917 mL | 3.4584 mL | 6.9168 mL | 17.2921 mL | |
| 10 mM | 0.3458 mL | 1.7292 mL | 3.4584 mL | 8.6460 mL | |
| 15 mM | 0.2306 mL | 1.1528 mL | 2.3056 mL | 5.7640 mL | |
| 20 mM | 0.1729 mL | 0.8646 mL | 1.7292 mL | 4.3230 mL | |
| 25 mM | 0.1383 mL | 0.6917 mL | 1.3834 mL | 3.4584 mL | |
| 30 mM | 0.1153 mL | 0.5764 mL | 1.1528 mL | 2.8820 mL | |
| 40 mM | 0.0865 mL | 0.4323 mL | 0.8646 mL | 2.1615 mL | |
| 50 mM | 0.0692 mL | 0.3458 mL | 0.6917 mL | 1.7292 mL | |
| 60 mM | 0.0576 mL | 0.2882 mL | 0.5764 mL | 1.4410 mL | |
| 80 mM | 0.0432 mL | 0.2162 mL | 0.4323 mL | 1.0808 mL | |
| 100 mM | 0.0346 mL | 0.1729 mL | 0.3458 mL | 0.8646 mL |