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Methyl-β-cyclodextrin, the randomly methylated form of β-cyclodextrin, is a cyclic heptasaccharide used to improve the water solubility of non-polar compounds such as fatty acids, lipids, vitamins and cholesterol for use in cell culture applications and to extract cholesterol from lipid membranes. As a cyclic heptasaccharide, it can also be used to deliver hydrophobic drugs based on its property of solubilizing non-polar substances. Methyl-β-cyclodextrin is also extensively used as a cholesterol-depleting reagent. Methyl-β-cyclodextrin strongly reduces clathrin-dependent endocytosis.
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ln Vitro |
For the purpose of enhancing the intake of tiny molecules like glucose and nanoparticles, methyl-β-cyclodextrin is widely employed to raise the permeability of cells[4]. Cyclodextrins are a kind of cyclic oligosaccharides that have a lipophilic core chamber and a hydrophilic outside. Generally speaking, cyclodextrin molecules do not penetrate lipophilic membranes since they are rather big molecules with many hydrogen sources and acceptors. The principal application of cyclodextrins in the pharmaceutical industry has been as complexing agents to improve the aqueous solubility, bioavailability, and stability of poorly soluble medicines. Drugs' bioavailability is one of the many uses for cyclodextrins in medicinal applications[4]. By rapidly removing cholesterol from the plasma membrane, methyl-β-cyclodextrin causes PEL cells to undergo caspase-dependent death. All PEL cell lines are inhibited in their development by methyl-β-cyclodextrin in a way that is dose dependent. Every cell line has an IC50 of 3.33–4.23 mM[5]. Among the several agents that deplete cholesterol from cells, methyl-β-cyclodextrin—a highly soluble cyclic heptasaccharide with a β glucopyranose unit—has been found to be the most efficient[5].
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ln Vivo |
Methyl-β-cyclodextrin effectively suppresses PEL cell growth and invasion in a PEL xenograft mice model without causing any evident side effects. Mice treated with methyl-β-cyclodextrin seem healthy, whereas those not treated have enlarged abdomens. The mice treated with methyl-β-cyclodextrin had significantly lower body weights than the control group. Mice treated with methyl-β-cyclodextrin had a much smaller volume of ascites than mice not treated with it[4]. Cyclodextrins have been found in studies on humans and animals to be useful in enhancing the distribution of nearly any kind of medication formulation. Around 30 distinct pharmaceutical products with drug/cyclodextrin complexes are available on the market at the moment[6] throughout the world.
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References |
[1]. Mundhara N, et al. Methyl-β-cyclodextrin, an actin depolymerizer augments the antiproliferative potential of microtubule-targeting agents. Sci Rep. 2019 May 21;9(1):7638.
[2]. Rodal SK, et al. Extraction of cholesterol with methyl-beta-cyclodextrin perturbs formation of clathrin-coated endocytic vesicles. Mol Biol Cell. 1999;10(4):961-974. [3]. Yuwei Huang, et al. Migrasome formation is mediated by assembly of micron-scale tetraspanin macrodomains. Nat Cell Biol. 2019 Aug;21(8):991-1002. [4]. Chen X, et al. Cholesterol depletion from the plasma membrane triggers ligand-independent activation of the epidermal growth factor receptor. J Biol Chem. 2002 Dec 20;277(51):49631-7. [5]. Gotoh K, et al. The antitumor effects of methyl-β-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. [6]. Tiwari G, et al. Cyclodextrins in delivery systems: Applications. J Pharm Bioallied Sci. 2010 Apr;2(2):72-9 |
Molecular Formula |
C54H94O35
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Molecular Weight |
1303.3032
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CAS # |
128446-36-6
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Appearance |
Typically exists as solids (or liquids in special cases) at room temperature
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SMILES |
[C@@H]12O[C@H]3O[C@@H]([C@@H](O[C@H]4O[C@@H]([C@@H](O[C@H]5O[C@@H]([C@@H](O[C@@H]6[C@@H](OC)[C@H](O)[C@@H]([C@@H](CO)O6)O[C@H]6O[C@H](CO)[C@H]([C@@H](OC)[C@@H]6OC)O[C@H]6O[C@H](CO)[C@H]([C@@H](OC)[C@@H]6OC)O[C@@H](O[C@@H]1CO)[C@@H](OC)[C@@H]2OC)[C@@H](O)[C@@H]5OC)CO)[C@@H](OC)[C@@H]4OC)CO)[C@@H](OC)[C@@H]3OC)CO
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HS Tariff Code |
2934.99.9001
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Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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Solubility (In Vitro) |
DMSO : ≥ 100 mg/mL
H2O : ≥ 50 mg/mL |
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Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80: Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 :Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400  (Please use freshly prepared in vivo formulations for optimal results.) |
Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
1 mM | 0.7673 mL | 3.8364 mL | 7.6728 mL | |
5 mM | 0.1535 mL | 0.7673 mL | 1.5346 mL | |
10 mM | 0.0767 mL | 0.3836 mL | 0.7673 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration: mg/mL;
Method for preparing DMSO stock solution: mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation::Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O,mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.