甲基-β-環(huán)糊精作用機(jī)制 - Medchemexpress - MCE中國(guó)

1、Product Data SheetMethyl-cyclodextrinCat. No.: HY-101461CAS No.: 128446-36-6作靶點(diǎn): Others作通路: Others儲(chǔ)存式: Powder -20C 3 years4C 2 yearsIn solvent -80C 6 months-20C 1 month溶解性數(shù)據(jù)體外實(shí)驗(yàn) DMSO : 100 mg/mLH2O : 50 mg/mL* means soluble, but saturation unknown.體內(nèi)實(shí)驗(yàn) 請(qǐng)根據(jù)您的實(shí)驗(yàn)動(dòng)物和給藥式選擇適當(dāng)?shù)娜芙獍?。以下溶解案都?qǐng)先按照 In Vitro 式配制澄清

2、的儲(chǔ)備液，再依次添加助溶劑：為保證實(shí)驗(yàn)結(jié)果的可靠性，澄 的儲(chǔ)備液可以根據(jù)儲(chǔ)存條件，適當(dāng)保存；體內(nèi)實(shí)驗(yàn)的作液，建議您現(xiàn)現(xiàn)配，當(dāng)天 使； 以下溶劑前顯的百分 指該溶劑在您配制終溶液中的體積占；如在配制過(guò)程中出現(xiàn)沉淀、析出現(xiàn)象，可 以通過(guò)加熱和/或超聲的式助溶1. 請(qǐng)依序添加每種溶劑： 10% DMSO 40% PEG300 5% Tween-80 45% salineSolubility: 2.75 mg/mL (Infinity mM); Clear solution此案可獲得 2.75 mg/mL (Infinity mM，飽和度未知) 的澄清溶液。以 1 mL 作液為例，取 100 L 27

3、.5 mg/mL 的澄 DMSO 儲(chǔ)備液加到 400 L PEG300 中，混合均勻；向上述體系中加50 L Tween-80，混合均勻；然后繼續(xù)加 450 L 理鹽定容 1 mL。2. 請(qǐng)依序添加每種溶劑： 10% DMSO 90% (20% SBE-CD in saline)Solubility: 2.75 mg/mL (Infinity mM); Clear solution此案可獲得 2.75 mg/mL (Infinity mM，飽和度未知) 的澄清溶液。以 1 mL 作液為例，取 100 L 27.5 mg/mL 的澄 DMSO 儲(chǔ)備液加到 900 L 20% 的 SBE-CD 理

4、鹽溶液中，混合均勻。3. 請(qǐng)依序添加每種溶劑： 10% DMSO 90% corn oilSolubility: 2.75 mg/mL (Infinity mM); Clear solution此案可獲得 2.75 mg/mL (Infinity mM，飽和度未知) 的澄 溶液，此案不適于實(shí)驗(yàn)周 期在半個(gè)以上的實(shí)驗(yàn)。以 1 mL 作液為例，取 100 L 27.5 mg/mL 的澄 DMSO 儲(chǔ)備液加到 900 L 油中，混合均勻。BIOLOGICAL ACTIVITY物活性Methyl-cyclodextrin (Methyl-beta-cyclodextrin) 種溶性環(huán)庚糖，對(duì)極性物質(zhì)有

5、增溶作，泛應(yīng)于疏Page 1 of 2 www.MedChemE性藥物的釋放。Methyl-cyclodextrin (Methyl-beta-cyclodextrin) 也泛作降膽固醇劑。體外研究 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.體內(nèi)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.戶使本產(chǎn)品發(fā)表的科研獻(xiàn) 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