甲基-β-环糊精作用机制 - Medchemexpress - MCE中国

1、Product Data SheetMethyl-cyclodextrinCat. No.: HY-101461CAS No.: 128446-36-6作靶点: Others作通路: Others储存式: Powder -20C 3 years4C 2 yearsIn solvent -80C 6 months-20C 1 month溶解性数据体外实验 DMSO : 100 mg/mLH2O : 50 mg/mL* means soluble, but saturation unknown.体内实验 请根据您的实验动物和给药式选择适当的溶解案。以下溶解案都请先按照 In Vitro 式配制澄清

2、的储备液，再依次添加助溶剂：为保证实验结果的可靠性，澄 的储备液可以根据储存条件，适当保存；体内实验的作液，建议您现现配，当天 使； 以下溶剂前显的百分 指该溶剂在您配制终溶液中的体积占；如在配制过程中出现沉淀、析出现象，可 以通过加热和/或超声的式助溶1. 请依序添加每种溶剂： 10% DMSO 40% PEG300 5% Tween-80 45% salineSolubility: 2.75 mg/mL (Infinity mM); Clear solution此案可获得 2.75 mg/mL (Infinity mM，饱和度未知) 的澄清溶液。以 1 mL 作液为例，取 100 L 27

3、.5 mg/mL 的澄 DMSO 储备液加到 400 L PEG300 中，混合均匀；向上述体系中加50 L Tween-80，混合均匀；然后继续加 450 L 理盐定容 1 mL。2. 请依序添加每种溶剂： 10% DMSO 90% (20% SBE-CD in saline)Solubility: 2.75 mg/mL (Infinity mM); Clear solution此案可获得 2.75 mg/mL (Infinity mM，饱和度未知) 的澄清溶液。以 1 mL 作液为例，取 100 L 27.5 mg/mL 的澄 DMSO 储备液加到 900 L 20% 的 SBE-CD 理

4、盐溶液中，混合均匀。3. 请依序添加每种溶剂： 10% DMSO 90% corn oilSolubility: 2.75 mg/mL (Infinity mM); Clear solution此案可获得 2.75 mg/mL (Infinity mM，饱和度未知) 的澄 溶液，此案不适于实验周 期在半个以上的实验。以 1 mL 作液为例，取 100 L 27.5 mg/mL 的澄 DMSO 储备液加到 900 L 油中，混合均匀。BIOLOGICAL ACTIVITY物活性Methyl-cyclodextrin (Methyl-beta-cyclodextrin) 种溶性环庚糖，对极性物质有

5、增溶作，泛应于疏Page 1 of 2 www.MedChemE性药物的释放。Methyl-cyclodextrin (Methyl-beta-cyclodextrin) 也泛作降胆固醇剂。体外研究 Methyl-cyclodextrin is extensively used to increase the permeability of cells, and thereby increase the uptake ofsmall molecules such as glucose and nano-particles2.Cyclodextrins are a family of cycli

6、c oligosaccharides with a hydrophilic outer surface and a lipophilic central cavity.Cyclodextrins molecules are relatively large with a number of hydrogen donors and acceptors and, thus in general,they do not permeate lipophilic membranes. In the pharmaceutical industry, cyclodextrins have mainly be

7、en used ascomplexing agents to increase aqueous solubility of poorly soluble drugs and to increase their bioavailability andstability. Cyclodextrins are used in pharmaceutical applications for numerous purposes, including improving thebioavailability of drugs2.Methyl-cyclodextrin quickly induces cas

8、pase-dependent apoptosis in PEL cells via cholesterol depletion from theplasma membrane. Methyl-cyclodextrin inhibits the growth of all PEL cell lines in a dose-dependent manner. The IC50 is 3.33-4.23 mM in each cell line3.Methyl-cyclodextrin is a highly water soluble cyclic heptasaccharide consisti

9、ng of a -glucopyranose unit, has beenreported as the most effective agent for the depletion of cholesterol from cells among the various cholesterol-depleting agents3.体内研究 In a PEL xenograft mouse model, Methyl-cyclodextrin significantly inhibits the growth and invasion of PEL cells without apparent

10、adverse effects. Methyl-cyclodextrin-treated mice appears to be healthy, whereas non-treated mice has a distended abdominal region. The body weights of control are significantly higher than those of Methyl-cyclodextrin treated mice. Methyl-cyclodextrin-treated mice has a significantly lower volume o

11、f ascites than that ofnon-treated mice3.Studies in both humans and animals have shown that cyclodextrins can be used to improve drug delivery from almostany type of drug formulation. Currently, there are approximately 30 different pharmaceutical products worldwidecontaining drug/cyclodextrins comple

12、xes in the market4.PROTOCOLCell Assay 1 PEL cells are incubated in triplicate in a 96-well microculture plate in the presence of different concentrations ofmethyl-cyclodextrin (0-10 mM) in a final volume of 0.1 mL for 24 h at 37C. Subsequently, MTT (0.5 mg/mL finalconcentration) is added to each wel

13、l. After 3 h of additional incubation, 100 L of a 0.04 N HCl is added to dissolvethe crystals. Absorption values at 570 nm are determined1.MCE has not independently confirmed the accuracy of these methods. They are for reference only.Animal Mice: Female NRJ mice are intraperitoneally inoculated with

14、 BCBL-1 cells suspended in PBS. The mice are thenAdministration 1 treated with intraperitoneal injections of PBS or methyl-cyclodextrin (500 mg/kg per day). Tumor burdens areevaluated by measuring body weights and ascites1.MCE has not independently confirmed the accuracy of these methods. They are f

15、or reference only.户使本产品发表的科研献 ACS Nano. 2020 Feb 25;14(2):2172-2182. Br J Pharmacol. 2020 Apr 15. J Biomed Nanotechnol. 2018 Dec 1;14(12):2114-2123. ACS Chem Biol. 2018 Nov 16;13(11):3078-3086. Toxicol Appl Pharmacol. 2019 Oct 1;380:114696.Page 2 of 3 www.MedChemESee more customer validations on HYP

16、ERLINK www.MedChemE www.MedChemEREFERENCES1. Gotoh K, et al. The antitumor effects of methyl-cyclodextrin against primary effusion lymphoma via the depletion of cholesterol from lipid rafts.Biochem Biophys Res Commun. 2014 Dec 12;455(3-4):285-9.2. Tiwari G, et al. Cyclodextrins in delivery systems:

17、Applications. J Pharm Bioallied Sci. 2010 Apr;2(2):72-9.3. Mundhara N, et al. Methyl-cyclodextrin, an actin depolymerizer augments the antiproliferative potential of microtubule-targeting agents. Sci Rep.2019 May 21;9(1):7638.4. Chen X, et al. Cholesterol depletion from the plasma membrane triggers ligand-independent activation of the epidermal growth factor receptor. J