| Size | Price | Stock | Qty |
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| 100mg |
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| 250mg |
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| 500mg |
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| 1g |
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Purity: ≥98%
Ciprofibrate (BRN-1984981; CCRIS 173; CCRIS173; Win-35833; BRN 1984981; BRN1984981;CCRIS-173) is a potent and selective agonist of PPAR/peroxisome proliferator-activated receptor agonist with antilipidemic activity. It was developed and approved in 1985 as a lipid-lowering agent. Ciprofibrate acts by activating PPARα with an EC50 value of 20 µM and only marginally affects PPARγ (EC50 = >300 µM). It has been shown to lower adipose tissue weight and reduce plasma insulin concentrations in obese rats and has been used clinically in the treatment of dyslipidemia.
| ln Vitro |
In rat Fao cells, ciprofibrate (500 μM; 4 hours) raises PPARa phosphorylation levels [1]. Ciprofibrate (10-100μM; 24 hours) promotes PPARR activation in rat liver H4IIEC3 cells transfected with the PPRE-AB LUC reporter plasmid, as demonstrated by the LucLite test [2]. HepG2 cells are not cytotoxic when exposed to ciprofibrate (10–100 μM) for a 24-hour period, and their viability is 99.7% [3]. In HepG2 cells, ciprofibrate (100 μM; 24 hours) likewise removed lipid deposition brought on by the FFA mixture and decreased the TG level that the FFA mixture had raised [3]. In HepG2 cells, ciprofibrate (100 μM; 24 h) nearly totally removed the FFA mixture-induced overproduction of inflammatory cytokines, such as MCP-1, TNF-α, and IL-6 [3].
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| ln Vivo |
Mice fed the MCD diet showed no discernible change in body weight or absolute liver weight when given ciprofibrate (oral; 10 mg/kg/day; 3 days). Mice on MCD diet benefit from ciprofibrate because it decreases hepatic necroinflammation and improves hepatic steatosis. In addition, it decreased the levels of hepatic cytokine protein and mRNA (MCP-1, TNFα, and IL-6) in comparison to mice given a diet lacking in choline [3].
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| Animal Protocol |
Animal/Disease Models: C57BL/6 mice (sixweeks old male) [3]
Doses: 10 mg/kg Route of Administration: Oral; 10 mg/kg/day; 3 days Experimental Results: MCD diet-induced liver steatosis and steatosis in mice Liver necrosis and inflammation are diminished. |
| 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.
[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. [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. |
| Molecular Formula |
C13H14CL2O3
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| Molecular Weight |
289.15
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| CAS # |
52214-84-3
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| Related CAS # |
Ciprofibrate-d6;2070015-05-1
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| SMILES |
ClC1(C([H])([H])C1([H])C1C([H])=C([H])C(=C([H])C=1[H])OC(C(=O)O[H])(C([H])([H])[H])C([H])([H])[H])Cl
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| InChi Key |
KPSRODZRAIWAKH-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C13H14Cl2O3/c1-12(2,11(16)17)18-9-5-3-8(4-6-9)10-7-13(10,14)15/h3-6,10H,7H2,1-2H3,(H,16,17)
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| Chemical Name |
2-(4-(2,2-dichlorocyclopropyl)phenoxy)-2-methylpropanoic acid
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| Synonyms |
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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 (8.65 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. Solubility in Formulation 2: ≥ 2.5 mg/mL (8.65 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 25.0 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. View More
Solubility in Formulation 3: ≥ 2.5 mg/mL (8.65 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 | 3.4584 mL | 17.2921 mL | 34.5841 mL | |
| 5 mM | 0.6917 mL | 3.4584 mL | 6.9168 mL | |
| 10 mM | 0.3458 mL | 1.7292 mL | 3.4584 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 |
| NCT03662984 | Completed | Drug: Ciprofibrate 100Mg Tablet Drug: Placebo Oral Tablet |
Myocardial Insulin Sensitivity Impaired Glucose Metabolism |
Maastricht University Medical Center | November 1, 2018 | Phase 3 |
| NCT00350038 | Completed | Drug: Irbesartan Drug: Ciprofibrate |
Hypertension Dyslipidemia |
Sanofi | February 2005 | Phase 4 |
| NCT03031821 | Terminated | Drug: Metformin Drug: Placebo Oral Tablet |
Prostate Cancer Metabolic Syndrome |
Canadian Urologic Oncology Group | July 12, 2018 | Phase 3 |
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