规格 | 价格 | 库存 | 数量 |
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10 mM * 1 mL in DMSO |
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100mg |
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250mg |
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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) |
在大鼠 Fao 细胞中,环丙贝特(500 μM;4 小时)可提高 PPARa 磷酸化水平 [1]。 LucLite 测试表明,环丙贝特(10-100μM;24 小时)可促进转染 PPRE-AB LUC 报告质粒的大鼠肝 H4IIEC3 细胞中 PPARR 的激活[2]。 HepG2 细胞暴露于环丙贝特 (10–100 μM) 24 小时后不会产生细胞毒性,其存活率为 99.7% [3]。在 HepG2 细胞中,环丙贝特(100 μM;24 小时)同样可以去除 FFA 混合物引起的脂质沉积,并降低 FFA 混合物升高的 TG 水平 [3]。在 HepG2 细胞中,环丙贝特(100 μM;24 小时)几乎完全消除了 FFA 混合物诱导的炎症细胞因子的过量产生,例如 MCP-1、TNF-α 和 IL-6 [3]。
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体内研究 (In Vivo) |
当给予环丙贝特(口服;10 毫克/公斤/天;3 天)时,喂食 MCD 饮食的小鼠体重或绝对肝脏重量没有明显变化。采用 MCD 饮食的小鼠受益于环丙贝特,因为它可以减少肝脏坏死炎症并改善肝脏脂肪变性。此外,与给予缺乏胆碱饮食的小鼠相比,它降低了肝细胞因子蛋白和 mRNA(MCP-1、TNFα 和 IL-6)的水平 [3]。
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动物实验 |
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. |
参考文献 |
[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. |
分子式 |
C13H14CL2O3
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分子量 |
289.15
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CAS号 |
52214-84-3
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相关CAS号 |
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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化学名 |
2-(4-(2,2-dichlorocyclopropyl)phenoxy)-2-methylpropanoic 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 (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. 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 | 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 |
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) 。
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NCT03031821 | Terminated | Drug: Metformin Drug: Placebo Oral Tablet |
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