| Size | Price | Stock | Qty |
|---|---|---|---|
| 25mg |
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| 50mg |
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| 100mg |
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| 250mg | |||
| Other Sizes |
| Targets |
Digitonin targets cholesterol molecules in cell membranes. By binding specifically to cholesterol, digitonin forms insoluble complexes that disrupt membrane integrity and increase permeability. This property makes digitonin a valuable tool for cell membrane permeabilization, allowing the introduction of molecules into cells or the extraction of cellular components. Digitonin's ability to increase cell permeability can enhance the efficacy of chemotherapeutic agents such as cisplatin and carboplatin.
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| ln Vitro |
In vitro, digitonin, a detergent that binds to cholesterol molecules in the cell membrane to promote permeability, has been shown to decrease tumor development and increase cisplatin accumulation[1].
In vitro, digitonin increases cell permeability by binding to cholesterol molecules in the cell membrane, which can increase cisplatin accumulation and reduce tumor growth. Digitonin is a natural glycoside detergent that can increase cell permeability by binding to cholesterol molecules and reduce tumor growth. It is used extensively as a mild non-ionic detergent for cell membrane permeabilization and subcellular fractionation. Digitonin finds application as a cholesterol precipitating agent. |
| ln Vivo |
The quantities are the same in the parenchyma of the liver. The tumor blood flow remains unchanged when Digitonin is measured using the 133Xe-clearance approach. When administered intra-aterially at 5 mg/kg of CBDCA, digitonin strengthens its tumor-growth-retarding properties, but not at 25 mg/kg [1].
In vivo, digitonin enhances the efficacy of carboplatin in liver tumors after intra-arterial administration. The compound's ability to increase cell permeability can improve the delivery and efficacy of chemotherapeutic agents. Digitonin has antitumor activity and can reduce tumor growth in animal models. However, digitonin is primarily used as a research tool rather than a therapeutic agent due to its non-specific membrane effects and potential toxicity. |
| Enzyme Assay |
In vitro enzyme/receptor binding assays for digitonin are not typical, as the compound is a detergent rather than a pharmacologically active agent. However, digitonin's ability to precipitate cholesterol can be assessed in vitro using cholesterol-containing liposomes or membranes. The compound's effects on membrane permeability can be measured using fluorescent dyes or radioactive tracers. Digitonin is commonly used in subcellular fractionation protocols to isolate organelles such as mitochondria and nuclei.
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| Cell Assay |
In vitro cell-based assays for digitonin evaluate its effects on cell membrane permeability and viability. Cells are cultured in appropriate media and treated with varying concentrations of digitonin. Cell membrane permeabilization is assessed using trypan blue exclusion or the uptake of fluorescent dyes such as propidium iodide. Cell viability is assessed using MTT or LDH release assays. The compound's ability to enhance the uptake and efficacy of chemotherapeutic agents such as cisplatin is evaluated in cancer cell lines.
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| Animal Protocol |
In vivo, digitonin is evaluated in animal models of cancer, where it is administered intra-arterially or intravenously in combination with chemotherapeutic agents such as carboplatin. Tumor growth is monitored, and the efficacy of the combination therapy is assessed. The compound's effects on tumor vascular permeability and drug delivery are evaluated. Pharmacokinetic studies are conducted to determine the compound's distribution and elimination.
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| ADME/Pharmacokinetics |
Digitonin is a natural product of the glycoside family and is a detergent. It has a molecular weight of 1229.31 g/mol. Digitonin is soluble in water and ethanol. The compound should be stored at room temperature. Digitonin is commonly used for cell membrane permeabilization and subcellular fractionation rather than as a therapeutic agent. It is a valuable tool for studying membrane biology and cell signaling.
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| Toxicity/Toxicokinetics |
The toxicity of digitonin is primarily associated with its membrane-disrupting properties. The compound can cause cell lysis and tissue damage at high concentrations. In animal studies, digitonin has been shown to have dose-dependent toxicity, with effects on the liver and kidneys. The compound should be handled with care in the laboratory, and appropriate safety measures should be taken to avoid exposure. For research use only, not for human use.
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| References |
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| Additional Infomation |
Crystals or white powder. (NTP, 1992)
Digitilloside has been reported to be found in foxglove, foxglove, and other organisms with relevant data. Digitilloside is a glycoside extracted from foxglove; its aglycone is digitigenyl, bound to five sugar molecules. Digitilloside can dissolve lipids, especially membrane lipids, and can be used as a cellular biochemical tool and a cholesterol precipitation reagent. It is harmless to the heart. Digitonin is a natural steroidal saponin and glycoside detergent obtained from Digitalis purpurea. It specifically binds to cholesterol in membranes, disrupting membrane integrity and increasing permeability. Digitonin is commonly used for cell membrane permeabilization and subcellular fractionation rather than as a therapeutic agent. It has antitumor activity and can increase cisplatin accumulation and reduce tumor growth in vitro. Digitonin enhances the efficacy of carboplatin in liver tumors after intra-arterial administration. |
| Molecular Formula |
C56H92O29
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|---|---|
| Molecular Weight |
1229.3123
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| Exact Mass |
1228.572
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| CAS # |
11024-24-1
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| PubChem CID |
6474107
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| Appearance |
Off-white to light yellow solid powder
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| Density |
1.6±0.1 g/cm3
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| Melting Point |
230-240ºC
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| Index of Refraction |
1.660
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| LogP |
-0.62
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| Hydrogen Bond Donor Count |
17
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| Hydrogen Bond Acceptor Count |
29
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| Rotatable Bond Count |
14
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| Heavy Atom Count |
85
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| Complexity |
2230
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| Defined Atom Stereocenter Count |
38
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| SMILES |
C[C@@H]1CC[C@@]2([C@H]([C@H]3[C@@H](O2)[C@H]([C@@H]4[C@@]3(CC[C@H]5[C@H]4CC[C@@H]6[C@@]5(C[C@H]([C@@H](C6)O[C@H]7[C@@H]([C@H]([C@H]([C@H](O7)CO)O[C@H]8[C@@H]([C@H]([C@@H]([C@H](O8)CO)O)O[C@H]9[C@@H]([C@H]([C@@H](CO9)O)O)O)O[C@H]2[C@@H]([C@H]([C@H]([C@H](O2)CO)O)O[C@H]2[C@@H]([C@H]([C@@H]([C@H](O2)CO)O)O)O)O)O)O)O)C)C)O)C)OC1
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| InChi Key |
UVYVLBIGDKGWPX-KUAJCENISA-N
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| InChi Code |
InChI=1S/C56H92O29/c1-19-7-10-56(75-17-19)20(2)31-45(85-56)37(67)32-22-6-5-21-11-26(24(61)12-55(21,4)23(22)8-9-54(31,32)3)76-50-42(72)39(69)44(30(16-60)80-50)81-53-48(47(36(66)29(15-59)79-53)83-49-40(70)33(63)25(62)18-74-49)84-52-43(73)46(35(65)28(14-58)78-52)82-51-41(71)38(68)34(64)27(13-57)77-51/h19-53,57-73H,5-18H2,1-4H3/t19-,20+,21+,22-,23+,24-,25-,26-,27-,28-,29-,30-,31+,32-,33+,34-,35+,36-,37+,38+,39-,40-,41-,42-,43-,44+,45-,46+,47+,48-,49+,50-,51+,52+,53+,54-,55+,56-/m1/s1
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| Chemical Name |
(2S,3R,4S,5S,6R)-2-[(2S,3R,4S,5S,6R)-2-[(2S,3R,4S,5R,6R)-2-[(2R,3R,4R,5R,6R)-6-[(1R,2S,3S,4R,5'R,6R,7S,8R,9S,12S,13S,15R,16R,18S)-3,15-dihydroxy-5',7,9,13-tetramethylspiro[5-oxapentacyclo[10.8.0.02,9.04,8.013,18]icosane-6,2'-oxane]-16-yl]oxy-4,5-dihydroxy-2-(hydroxymethyl)oxan-3-yl]oxy-5-hydroxy-6-(hydroxymethyl)-4-[(2S,3R,4S,5R)-3,4,5-trihydroxyoxan-2-yl]oxyoxan-3-yl]oxy-3,5-dihydroxy-6-(hydroxymethyl)oxan-4-yl]oxy-6-(hydroxymethyl)oxane-3,4,5-triol
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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 Note: Please store this product in a sealed and protected environment (e.g. under nitrogen), avoid exposure to moisture. |
| 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) |
H2O : ~100 mg/mL (~81.35 mM)
DMSO : ~100 mg/mL (~81.35 mM) |
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 25 mg/mL (20.34 mM) (saturation unknown) in PBS (add these co-solvents sequentially from left to right, and one by one), clear solution.
(Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 0.8135 mL | 4.0673 mL | 8.1346 mL | |
| 5 mM | 0.1627 mL | 0.8135 mL | 1.6269 mL | |
| 10 mM | 0.0813 mL | 0.4067 mL | 0.8135 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.
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