Tocofersolan
(Synonyms: 维生素E聚乙二醇琥珀酸酯,TPGS; D-α-Tocopherol polyethylene glycol 1000 succinate; Vitamin E-TPGS) 目录号 : GC31315
Tocofersolan是α-生育酚的聚乙二醇衍生物，是一种水溶性的维生素E类似物。
Cas No.:9002-96-4
Sample solution is provided at 25 µL, 10mM.
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Tocofersolan is a polyethylene glycol derivative of α-tocopherol and is a water-soluble vitamin E analog[1]. Tocofersolan has antioxidant activity and serves as an orally bioavailable source of vitamin E[2]. Tocofersolan increases the solubility and bioavailability of some drugs, and improves their pharmacokinetic properties[3]. Tocofersolan is usually used in drug delivery systems or nutraceuticals[4][5].
In vitro, Tocofersolan (3.3µM to 16.5mM; 60min) inhibited P-glycoprotein (P-gp) - mediated drug efflux in Caco-2 cells with an IC50 of 5.86µM[6].
In vivo, Tocofersolan (1µM) co-exposure for 5 days post-fertilization in larval zebrafish reversed the locomotor hypoactivity caused by benzo[a]pyrene (5µM) exposure[7].
References:
[1] Sadoqi M, Lau-Cam CA, Wu SH. Investigation of the micellar properties of the tocopheryl polyethylene glycol succinate surfactants TPGS 400 and TPGS 1000 by steady state fluorometry. J Colloid Interface Sci. 2009;333(2):585-589.
[2] Thebaut A, Nemeth A, Le Mouhaer J, et al. Oral Tocofersolan Corrects or Prevents Vitamin E Deficiency in Children With Chronic Cholestasis. J Pediatr Gastroenterol Nutr. 2016;63(6):610-615.
[3] Wande DP, Cui Q, Chen S, Xu C, Xiong H, Yao J. Rediscovering Tocophersolan: A Renaissance for Nano-Based Drug Delivery and Nanotheranostic Applications. Curr Drug Targets. 2021;22(8):856-869.
[4] Tan S, Zou C, Zhang W, Yin M, Gao X, Tang Q. Recent developments in d-α-tocopheryl polyethylene glycol-succinate-based nanomedicine for cancer therapy. Drug Deliv. 2017;24(1):1831-1842.
[5] Srivastava A, Lall R, Talukder J, DuBourdieu D, Gupta RC. Iron Transport Tocopheryl Polyethylene Glycol Succinate in Animal Health and Diseases. Molecules. 2019;24(23):4289.
[6] Collnot EM, Baldes C, Wempe MF, et al. Mechanism of inhibition of P-glycoprotein mediated efflux by vitamin E TPGS: influence on ATPase activity and membrane fluidity. Mol Pharm. 2007;4(3):465-474.
[7] Holloway Z, Hawkey A, Asrat H, Boinapally N, Levin ED. The use of tocofersolan as a rescue agent in larval zebrafish exposed to benzo[a]pyrene in early development. Neurotoxicology. 2021;86:78-84.
Tocofersolan是α-生育酚的聚乙二醇衍生物，是一种水溶性的维生素E类似物[1]。Tocofersolan具有抗氧化活性，可作为维生素E的口服生物可利用来源[2]。Tocofersolan能够增加某些药物的溶解度和生物利用度，从而改善药物的药代动力学特性[3]。Tocofersolan常用于药物递送系统或营养保健品中[4][5]。
体外实验中，Tocofersolan（3.3µM-16.5mM；60分钟）在Caco-2 细胞中抑制了 P-糖蛋白（P-gp）介导的药物外排，IC50值为5.86µM[6]。
体内实验中，斑马鱼幼虫受精后5天暴露于Tocofersolan（1µM）可逆转苯并[a]芘（5µM）暴露引起的运动能力低下[7]。
| Cell experiment [1]: | |
Cell lines | Caco-2 cells |
Preparation Method | Caco-2 cells were grown to 90% confluence in 75cm2 T-flasks with DMEM supplemented with 10% FBS and 1% NEAA. Culture media were changed every second day, and cells were grown at a temperature of 37°C in an atmosphere of 85% relative humidity and 5% CO2. Trypsinized Caco-2 cells were spin labeled by incubating a suspension (2.0×107 cells/mL) in Krebs Ringer Buffer (KRB; pH 7.4) for 30min at 37°C with 0.5mM of a spin label stock solution (10mM 5-doxyl stearic acid (5-SA) in ethanol). Different concentrations of Tocofersolan (3.3µM to 16.5mM) were added via stock solutions, and cell suspensions were incubated for 60min. After suspension centrifugation (4min at 1200g), supernatant was removed and the cell pellet was washed and resuspended in KRB to give a final concentration of 1.0×108 cells/mL. To quench residual free spin label, chrome oxalate (final concentration 2.0mM) was added and the ensuing cell suspension (100µL) was filled into the test tube and placed in a 4103 TM/ 8609 cavity. ESR measurements were performed at room temperature using a Bruker ESP300 E spectrometer with an ER081 (90/30 C5) magnet. Cell membrane fluidity was depicted via the cell membrane order parameter S. S can be derived from the ESR spectral line splitting. |
Reaction Conditions | 3.3µM to 16.5mM; 60min |
Applications | Tocofersolan had negligible effects on Caco-2 cell membrane fluidity at concentrations up to 0.33mM, but significant fluidization effects were observed at higher concentrations (above 1.65mM). |
References: | |
| Cas No. | 9002-96-4 | SDF | |
| 别名 | 维生素E聚乙二醇琥珀酸酯,TPGS; D-α-Tocopherol polyethylene glycol 1000 succinate; Vitamin E-TPGS | ||
| Canonical SMILES | CC1=C(CCC(CCCC(C)CCCC(C)CCCC(C)C)(C)O2)C2=C(C)C(C)=C1OC(CCC(OCCO)=O)=O.[n] | ||
| 分子式 | C35H58O6 | 分子量 | 1513.00 |
| 溶解度 | DMSO : 31.25 mg/mL (20.65 mM);Water : < 0.1 mg/mL (insoluble) | 储存条件 | Store at -20°C |
| General tips | 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。 储备液的保存方式和期限：-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 660.9 μL | 3.3047 mL | 6.6094 mL |
| 5 mM | 132.2 μL | 660.9 μL | 1.3219 mL |
| 10 mM | 66.1 μL | 330.5 μL | 660.9 μL |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
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，
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 saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
3. 以上所有助溶剂都可在 GlpBio 网站选购。
Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet