规格 | 价格 | 库存 | 数量 |
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10 mM * 1 mL in DMSO |
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50mg |
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100mg |
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500mg |
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1g |
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Other Sizes |
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体外研究 (In Vitro) |
Bezafibrate 是一种 PPAR 激动剂。对于小鼠 PPARα、PPARγ 和 PPARδ,相应的 EC50 值为 90 μM、55 μM 和 110 μM。人 PPARα、PPARγ 和 PPARδ 的 EC50 值分别为 50 μM、60 μM 和 20 μM。是[1]。当应用于人视网膜色素上皮 ARPE-19 细胞和人视网膜微血管内皮细胞 (HRMEC) 时,苯扎贝特 (>200 μM) 表现出显着的细胞毒性。在 HRMEC 中,bezafibrate (30-100 μM) 可减少 TNFα 诱导的炎症因子并控制 TNFα 诱导的核因子 (NF)-κB 反式激活。 Bezafibrate 抑制 VEGF 引起的 HRMEC 迁移以及白细胞介素 (IL)-1β 刺激的 ARPE-19 细胞释放 VEGF [2]。
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体内研究 (In Vivo) |
在 TallyHo 小鼠中,苯扎贝特 (0.5%) 显着降低血浆脂质和葡萄糖水平,并增加胰岛的大小。苯扎贝特还可以增强代谢灵活性和能量消耗。苯扎贝特还可以增强脂肪变性,改变脂质的组成,并增加肝脏中线粒体的质量[3]。
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动物实验 |
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参考文献 |
[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 |
分子式 |
C19H20CLNO4
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分子量 |
361.82
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CAS号 |
41859-67-0
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相关CAS号 |
Bezafibrate-d6;1219802-74-0;Bezafibrate-d4;1189452-53-6
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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
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InChi Key |
IIBYAHWJQTYFKB-UHFFFAOYSA-N
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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)
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化学名 |
2-[4-[2-[(4-chlorobenzoyl)amino]ethyl]phenoxy]-2-methyl-propanoic acid
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别名 |
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存储方式 |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
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运输条件 |
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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溶解度 (体外) |
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溶解度 (体内) |
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. 1、请先配制澄清的储备液(如:用DMSO配置50 或 100 mg/mL母液(储备液)); 2、取适量母液,按从左到右的顺序依次添加助溶剂,澄清后再加入下一助溶剂。以 下列配方为例说明 (注意此配方只用于说明,并不一定代表此产品 的实际溶解配方): 10% DMSO → 40% PEG300 → 5% Tween-80 → 45% ddH2O (或 saline); 假设最终工作液的体积为 1 mL, 浓度为5 mg/mL: 取 100 μL 50 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中,混合均匀/澄清;向上述体系中加入50 μL Tween-80,混合均匀/澄清;然后继续加入450 μL ddH2O (或 saline)定容至 1 mL; 3、溶剂前显示的百分比是指该溶剂在最终溶液/工作液中的体积所占比例; 4、 如产品在配制过程中出现沉淀/析出,可通过加热(≤50℃)或超声的方式助溶; 5、为保证最佳实验结果,工作液请现配现用! 6、如不确定怎么将母液配置成体内动物实验的工作液,请查看说明书或联系我们; 7、 以上所有助溶剂都可在 Invivochem.cn网站购买。 |
制备储备液 | 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 |
1、根据实验需要选择合适的溶剂配制储备液 (母液):对于大多数产品,InvivoChem推荐用DMSO配置母液 (比如:5、10、20mM或者10、20、50 mg/mL浓度),个别水溶性高的产品可直接溶于水。产品在DMSO 、水或其他溶剂中的具体溶解度详见上”溶解度 (体外)”部分;
2、如果您找不到您想要的溶解度信息,或者很难将产品溶解在溶液中,请联系我们;
3、建议使用下列计算器进行相关计算(摩尔浓度计算器、稀释计算器、分子量计算器、重组计算器等);
4、母液配好之后,将其分装到常规用量,并储存在-20°C或-80°C,尽量减少反复冻融循环。
计算结果:
工作液浓度: mg/mL;
DMSO母液配制方法: mg 药物溶于 μL DMSO溶液(母液浓度 mg/mL)。如该浓度超过该批次药物DMSO溶解度,请首先与我们联系。
体内配方配制方法:取 μL DMSO母液,加入 μL PEG300,混匀澄清后加入μL Tween 80,混匀澄清后加入 μL ddH2O,混匀澄清。
(1) 请确保溶液澄清之后,再加入下一种溶剂 (助溶剂) 。可利用涡旋、超声或水浴加热等方法助溶;
(2) 一定要按顺序加入溶剂 (助溶剂) 。
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> |