Size | Price | Stock | Qty |
---|---|---|---|
100mg |
|
||
500mg |
|
||
1g |
|
||
Other Sizes |
|
Bezafibrate (BM 15075; BM-15075; Benzofibrate; BM15075; Bezalip; Bezatrol; Difaterol; Cedur; Bezafibratum) is an anti-hypertriglyceridemic/lipid-lowering drug acting. It acts as a potent agonist of PPAR (peroxisome proliferator-activated receptor alpha) with EC50s of 50 μM, 60 μM, 20 μM for human PPARα, PPARγ and PPARδ.
ln Vitro |
Bezafibrate is a PPAR agonist. For mouse PPARα, PPARγ, and PPARδ, the corresponding EC50 values are 90 μM, 55 μM, and 110 μM. Human PPARα, PPARγ, and PPARδ have respective EC50 values of 50 μM, 60 μM, and 20 μM. is [1]. When applied to human retinal pigment epithelial ARPE-19 cells and human retinal microvascular endothelial cells (HRMEC), bezafibrate (>200 μM) exhibits notable cytotoxicity. In HRMEC, bezafibrate (30-100 μM) reduces TNFα-induced inflammatory factors and controls TNFα-induced nuclear factor (NF)-κB transactivation. Bezafibrate inhibits the migration of HRMECs caused by VEGF and the release of VEGF by ARPE-19 cells stimulated by interleukin (IL)-1β [2].
|
||
---|---|---|---|
ln Vivo |
In TallyHo mice, bezafibrate (0.5%) markedly decreased plasma lipid and glucose levels and increased the size of the pancreatic islet. Bezafibrate also enhances metabolic flexibility and energy expenditure. Bezafibrate also enhances steatosis, modifies the makeup of lipids, and boosts the mass of mitochondria in the liver [3].
|
||
Animal Protocol |
|
||
References |
[1]. Willson TM, et al. The PPARs: from orphan receptors to drug discovery. J Med Chem. 2000 Feb 24;43(4):527-50.
[2]. Usui-Ouchi A, et al. The peroxisome proliferator-activated receptor pan-agonist bezafibrate suppresses microvascular inflammatory responses of retinal endothelial cells and vascular endothelial growth factor production in retinal pigmented epithelial cells. Int Immunopharmacol. 2017 Nov;52:70-76. [3]. Franko A, et al. Bezafibrate ameliorates diabetes via reduced steatosis and improved hepatic insulin sensitivity in diabetic TallyHo mice. Mol Metab. 2017 Jan 6;6(3):256-266 |
Molecular Formula |
C19H20CLNO4
|
|
---|---|---|
Molecular Weight |
361.82
|
|
CAS # |
41859-67-0
|
|
Related CAS # |
Bezafibrate-d6;1219802-74-0;Bezafibrate-d4;1189452-53-6
|
|
SMILES |
ClC1C([H])=C([H])C(=C([H])C=1[H])C(N([H])C([H])([H])C([H])([H])C1C([H])=C([H])C(=C([H])C=1[H])OC(C(=O)O[H])(C([H])([H])[H])C([H])([H])[H])=O
|
|
InChi Key |
IIBYAHWJQTYFKB-UHFFFAOYSA-N
|
|
InChi Code |
InChI=1S/C19H20ClNO4/c1-19(2,18(23)24)25-16-9-3-13(4-10-16)11-12-21-17(22)14-5-7-15(20)8-6-14/h3-10H,11-12H2,1-2H3,(H,21,22)(H,23,24)
|
|
Chemical Name |
2-[4-[2-[(4-chlorobenzoyl)amino]ethyl]phenoxy]-2-methyl-propanoic acid
|
|
Synonyms |
|
|
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)
|
Solubility (In Vitro) |
|
|||
---|---|---|---|---|
Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (6.91 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 (6.91 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (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 corn oil and mix evenly. View More
Solubility in Formulation 3: 10 mg/mL (27.64 mM) in 0.5% CMC-Na/saline water (add these co-solvents sequentially from left to right, and one by one), suspension solution; with ultrasonication. |
Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
1 mM | 2.7638 mL | 13.8190 mL | 27.6381 mL | |
5 mM | 0.5528 mL | 2.7638 mL | 5.5276 mL | |
10 mM | 0.2764 mL | 1.3819 mL | 2.7638 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 |
NCT04309773 | Recruiting | Drug: Bezafibrate (400mg) in addition to standard 15-20 mg/kg/jour UDCA therapy |
Primary Sclerosing Cholangitis Cholestasis |
Assistance Publique - Hôpitaux de Paris | April 6, 2021 | Phase 3 |
NCT02548832 | Completed Has Results | Drug: Bezafibrate Drug: Berberine plus Bezafibrate |
Mixed Dyslipidemia | University of Guadalajara | April 2013 | Phase 3 |
NCT02291796 | Completed | Drug: Bezafibrate | Acute Myocardial Infarction | Instituto Mexicano del Seguro Social | January 2011 | Phase 4 |
NCT02398201 | Completed | Drug: Bezafibrate | Mitochondrial Diseases | Newcastle-upon-Tyne Hospitals NHS Trust |
September 2015 | Phase 2 |
Pancreas architecture. A. Pancreata were stained with anti-insulin (green) and anti-glucagon (red) antibodies and visualized by fluorescence microscopy. Cell nuclei were stained with DAPI (blue). The white bar represents 50 μm. Representative areas are shown. B. Insulin area normalized to islet area and C. total insulin area normalized to pancreas area were calculated using Architect software. D. Islet number was manually counted and values were normalized to total pancreas area. Columns represent averages ± standard deviations; n = 5. *denotes significant differences between ED, BEZ vs. ED, SD; *p < 0.05, **p < 0.01; #denotes significant differences between ED, SD vs. LD, SD; ##p < 0.01; §denotes significant differences between LD, BEZ vs. LD, SD; §§p < 0.01. td> |
Body composition and indirect calorimetry. A. Body weight. B. Fat and C. lean mass were measured by qNMR (Suppl. Figure 3A,B) and normalized to body weights in %. D. Average oxygen consumption normalized to body weights. E. Respiratory exchange ratios (RERs) were calculated by dividing carbon dioxide production (VCO2) by oxygen consumption (VO2) (Suppl. Figure 4A–D). The gray rectangle represents 12-h dark phase (0-time point represents 1 p.m.). F. ΔRER was calculated as RERmax − RERmin. Columns represent averages ± standard deviations; n = 8–12. *denotes significant differences between ED, BEZ vs. ED, SD; *p < 0.05, **p < 0.01, ***p < 0.001; #denotes significant differences between ED, SD vs. LD, SD; #p < 0.05, ###p < 0.001; §denotes significant differences between LD, BEZ vs. LD, SD; §§p < 0.01, §§§p < 0.001. td> |
Euglycemic-hyperinsulinemic clamp. A. Steady state BG levels during the clamp. B. Glucose infusion rate (GINF). C. Endogenous glucose production (EGP). D. Whole body glucose uptake. Columns represent averages ± standard deviations; n = 8 animals. §denotes significant differences between LD, BEZ vs. LD, SD; §p < 0.05, §§§p < 0.001. td> |