(2-Hydroxypropyl)-β-cyclodextrin(Synonyms: 羟丙基-β-环糊精; Hydroxypropyl betadex; Hydroxypropyl-β-cyclodextrin; HP-β-CD)

(2-Hydroxypropyl)-β-cyclodextrin (Synonyms: 羟丙基-β-环糊精; Hydroxypropyl betadex; Hydroxypropyl-β-cyclodextrin; HP-β-CD)

(2-Hydroxypropyl)-β-cyclodextrin是广泛使用的药物递送载体,可提高稳定性和利用度。

(2-Hydroxypropyl)-β-cyclodextrin(Synonyms: 羟丙基-β-环糊精; Hydroxypropyl betadex;  Hydroxypropyl-β-cyclodextrin;  HP-β-CD)

(2-Hydroxypropyl)-β-cyclodextrin Chemical Structure

CAS No. : 128446-35-5

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生物活性

(2-Hydroxypropyl)-β-cyclodextrin is a widely used drug delivery vehicle to improve the stability and bioavailability.

体外研究
(In Vitro)

Cell treatment with (2-Hydroxypropyl)-β-cyclodextrin results in the activation of the transcription factor EB, a master regulator of lysosomal function and autophagy, and in enhancement of the cellular autophagic clearance capacity[1]. (2-Hydroxypropyl)-β-cyclodextrin treatment reduces intracellular cholesterol resulting in significant leukemic cell growth inhibition through G2/M cell-cycle arrest and apoptosis. The IC50 values for (2-Hydroxypropyl)-β-cyclodextrin after 72 hours exposure are in the range of 3.86–10.09 mM. (2-Hydroxypropyl)-β-cyclodextrin also shows anticancer effects against CML cells expressing a T315I BCR-ABL mutation (that confers resistance to most ABL tyrosine kinase inhibitors), and hypoxia-adapted CML cells that have characteristics of leukemic stem cells. In addition, colony forming ability of human primary AML and CML cells is inhibited by (2-Hydroxypropyl)-β-cyclodextrin[2].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

体内研究
(In Vivo)

(2-Hydroxypropyl)-β-cyclodextrin administration promotes transcription factor EB-mediated clearance of proteolipid aggregates that accumulate due to inefficient activity of the lysosome-autophagy system in cells derived from a patient with a lysosomal storage disorder[1]. Intraperitoneal injection of (2-Hydroxypropyl)-β-cyclodextrin significantly improves survival in leukemia mouse models. Systemic administration of (2-Hydroxypropyl)-β-cyclodextrin to mice has no significant adverse effects[2].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Clinical Trial

CAS 号

128446-35-5

中文名称

羟丙基-β-环糊精

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
溶解性数据
In Vitro: 

DMSO : 50 mg/mL (Need ultrasonic)

H2O : 50 mg/mL (Need ultrasonic)

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液,再依次添加助溶剂:

——为保证实验结果的可靠性,澄清的储备液可以根据储存条件,适当保存;体内实验的工作液,建议您现用现配,当天使用; 以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比;如在配制过程中出现沉淀、析出现象,可以通过加热和/或超声的方式助溶

  • 1.

    请依序添加每种溶剂: Saline

    Solubility: 200 mg/mL (Infinity mM); Clear solution; Need ultrasonic

  • 2.

    请依序添加每种溶剂: 10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 2.08 mg/mL (Infinity mM); Clear solution

    此方案可获得 ≥ 2.08 mg/mL (Infinity mM,饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例,取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中,混合均匀;向上述体系中加入50 μL Tween-80,混合均匀;然后继续加入 450 μL生理盐水定容至 1 mL。

    将 0.9 g 氯化钠,完全溶解于 100 mL ddH₂O 中,得到澄清透明的生理盐水溶液

  • 3.

    请依序添加每种溶剂: 10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: ≥ 2.08 mg/mL (Infinity mM); Clear solution

    此方案可获得 ≥ 2.08 mg/mL (Infinity mM,饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例,取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液中,混合均匀。

    将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中,再用生理盐水定容至 10 mL,完全溶解,澄清透明
  • 4.

    请依序添加每种溶剂: 10% DMSO    90% corn oil

    Solubility: ≥ 2.08 mg/mL (Infinity mM); Clear solution

    此方案可获得 ≥ 2.08 mg/mL (Infinity mM,饱和度未知) 的澄清溶液,此方案不适用于实验周期在半个月以上的实验。

    以 1 mL 工作液为例,取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中,混合均匀。

*以上所有助溶剂都可在 MCE 网站选购。
参考文献
  • [1]. Song W, et al. 2-Hydroxypropyl-β-cyclodextrin promotes transcription factor EB-mediated activation of autophagy: implications for therapy. J Biol Chem. 2014 Apr 4;289(14):10211-22.

    [2]. Yokoo M, et al. 2-Hydroxypropyl-β-Cyclodextrin Acts as a Novel Anticancer Agent. PLoS One. 2015 Nov 4;10(11):e0141946.

Cell Assay
[2]

Cells are incubated with (2-Hydroxypropyl)-β-cyclodextrin at various concentrations (5, 7.5, 10, 15, 20 mM) for 72 hours. Cell viability is assessed using a trypan blue dye exclusion method and cell proliferation is evaluated using a modified methyl-thiazol-diphenyl- tetrazolium (MTT) assay[2].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Administration
[2]

Mice: Mice are intraperitoneally injected with 200 μL vehicle (saline) or (2-Hydroxypropyl)-β-cyclodextrin (50 or 150 mM) for 20 consecutive days 3 days after transplantation, and survival is monitored daily. Leukemic cell engraftment is confirmed by detection of GFP-positive cells in the recipient’s BM using flow cytometry[2].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

参考文献
  • [1]. Song W, et al. 2-Hydroxypropyl-β-cyclodextrin promotes transcription factor EB-mediated activation of autophagy: implications for therapy. J Biol Chem. 2014 Apr 4;289(14):10211-22.

    [2]. Yokoo M, et al. 2-Hydroxypropyl-β-Cyclodextrin Acts as a Novel Anticancer Agent. PLoS One. 2015 Nov 4;10(11):e0141946.