PEG300 (Glycols polyethylene)
(Synonyms: 聚乙二醇) 目录号 : GC30022
PEG-300是一种中性聚合物，分子量为300，由乙二醇重复单元形成。
Cas No.:25322-68-3
Sample solution is provided at 25 µL, 10mM.
PEG-300, a neutral polymer with a molecular weight of 300, is a water-soluble, low immunogenic and biocompatible polymer formed by repeating units of ethylene glycol [1，2].
Relatively high but clinically achievable PEG-300 levels can inhibit P-gp activity in Caco-2 cell monolayers, thereby enhancing the permeability of anticancer drugs such as paclitaxel and doxorubicin. For example, increasing the concentration of PEG-300 will lead to the increase of Papp and AP to BL of [3H] paclitaxel [P-gp substrate][3-6]12-14,28 and the decrease of Papp and BL to AP. At high concentrations (20%, v/v) of peg-300, it seems that paclitaxel is transported across Caco-2 cell monolayers by simple passive transcellular diffusion. Similar peg induced inhibition of efflux transporters (e.g., P-gp and / or P-gp / MRP activity) was observed in Caco-2 cells, [5] doxorubicin, indicating that PEG induced inhibition of efflux is not a unique phenomenon of paclitaxel.
References:
[1] Lee C C, Su Y C, Ko T P, et al. Structural basis of polyethylene glycol recognition by antibody[J]. Journal of biomedical science, 2020, 27(1): 1-13.
[2] Billingham J, Breen C, Yarwood J. Adsorption of polyamine, polyacrylic acid and polyethylene glycol on montmorillonite: An in situ study using ATR-FTIR[J]. Vibrational Spectroscopy, 1997, 14(1): 19-34.
[3] Krishna R, Mayer L D. Multidrug resistance (MDR) in cancer: mechanisms, reversal using modulators of MDR and the role of MDR modulators in influencing the pharmacokinetics of anticancer drugs[J]. European Journal of Pharmaceutical Sciences, 2000, 11(4): 265-283.
[4] Van Asperen J, Van Tellingen O, Sparreboom A, et al. Enhanced oral bioavailability of paclitaxel in mice treated with the P-glycoprotein blocker SDZ PSC 833[J]. British Journal of Cancer, 1997, 76(9): 1181-1183.
[5] van Asperen J, van Tellingen O, van der Valk M A, et al. Enhanced oral absorption and decreased elimination of paclitaxel in mice cotreated with cyclosporin A[J]. Clinical cancer research: an official journal of the American Association for Cancer Research, 1998, 4(10): 2293-2297.
PEG-300是一种中性聚合物,分子量为300,由乙二醇重复单元形成。它是水溶性、低免疫原性和生物相容性的聚合物。
相对较高但在临床上可达到的PEG-300水平可以抑制Caco-2细胞单层中P-gp活性,从而增强像紫杉醇和多柔比星等抗癌药物的渗透性。例如,增加PEG-300浓度将导致[3H]紫杉醇[P-gp底物]的Papp和AP to BL[3-6]12-14,28增加,并降低Papp和BL to AP。在高浓度（20％v/v）的PEG-300下,似乎紫杉醇通过简单的跨细胞膜扩散被运输穿过Caco-2细胞单层。类似地,在Caco-2细胞中观察到了peg诱导外流转运体（如P-gp和/或P-gp/MRP活性）的抑制作用[5]多柔比星,表明PEG诱导外流阻滞不是紫杉醇独有现象。
| Cell experiment [1]: | |
|
Cell lines |
Caco-2 cells |
|
Preparation Method |
When Caco-2 cells were added, 1.5 ml of complete medium was added to the top [apical (AP) compartment] and 2.6 ml to the bottom [basolateral (BL) compartment] of each transwell1. The P-gp activity in these cell monolayers was routinely evaluated by bidirectional transport studies of the P-gp substrate [3H] paclitaxel. |
|
Reaction Conditions |
0/20% for 3h |
|
Applications |
The AP-to-BL flux of testosterone (0.3 mM) across Caco-2 cell monolayers was determined in the absence and presence of the highest concentration (20%, v/v) of PEG-300 used in these studies to test any possible effects of this excipient on the passive transcellular pathway across Caco2 cells.33 The experimental results suggest that PEG-300 does not alter the passive transcellular pathway across Caco-2 cell monolayers. |
|
References: [1]. Hugger E D, Audus K L, Borchardt R T. Effects of poly (ethylene glycol) on efflux transporter activity in Caco©\2 cell monolayers[J]. Journal of pharmaceutical sciences, 2002, 91(9): 1980-1990. |
|
| Cas No. | 25322-68-3 | SDF | |
| 别名 | 聚乙二醇 | ||
| Canonical SMILES | OCCCCOC[H].[n] | ||
| 分子式 | H(OCH2CH2)nOH | 分子量 | 300.00 |
| 溶解度 | DMSO : 100 mg/mL (960.15 mM);Water : ≥ 50 mg/mL (480.08 mM) | 储存条件 | Store at RT |
| 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。 |
||
| 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 | |||
 |
1 mg | 5 mg | 10 mg |
| 1 mM | 3.3333 mL | 16.6667 mL | 33.3333 mL |
| 5 mM | 0.6667 mL | 3.3333 mL | 6.6667 mL |
| 10 mM | 0.3333 mL | 1.6667 mL | 3.3333 mL |
| 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