| Size | Price | Stock | Qty |
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| 100mg |
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| 250mg | |||
| Other Sizes |
| Targets |
Tubeimoside I has multiple molecular targets. It is an orally active HSPD1 (heat shock protein family D member 1) inhibitor. It also inhibits NF-κB and MAPK signaling pathways, and regulates the eNOS-VEGF pathway. Furthermore, it has been reported to bind to tubulin at the colchicine site, inhibiting microtubule polymerization. This multi-targeting ability contributes to its diverse pharmacological effects, including the induction of apoptosis and autophagy.
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| ln Vitro |
In vitro, tubeimoside I demonstrates potent anticancer activity against a wide range of cancer cell lines, including those from liver, lung, colorectal, cervical, breast, and nasopharyngeal cancers. It induces cytoprotective autophagy in human breast cancer cells via an Akt-mediated pathway. It also inhibits the viability of cervical cancer and colon cancer cells in a dose-dependent manner. Additionally, it attenuates LPS-induced inflammation in RAW 264.7 cells by inhibiting the production of pro-inflammatory cytokines like TNF-α, IL-6, and IL-1β.
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| ln Vivo |
In vivo, tubeimoside I has shown significant anti-tumor efficacy in mouse xenograft models. Intraperitoneal administration inhibited the growth of tumors in nude mice without causing a decrease in body weight. It also reduced lung injury and down-regulated the secretion of inflammatory cytokines in a murine model of LPS-induced acute lung injury. Oral administration has also been shown to attenuate inflammation and oxidative damage in mice.
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| Enzyme Assay |
In vitro enzyme or receptor binding (non-cell) assays for tubeimoside I involve studying its interaction with purified proteins. For example, its inhibition of HSPD1 can be measured using a biochemical assay where the chaperone activity of HSPD1 is monitored in the presence of the compound. Its binding to tubulin at the colchicine site can be assessed using a competition binding assay with [³H]colchicine. The activity of kinases in the NF-κB or MAPK pathways can also be tested using purified enzymes and specific peptide substrates.
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| Cell Assay |
In vitro cell-based assays for tubeimoside I are performed using various cancer cell lines. Cells are treated with the compound at different concentrations for 24 to 72 hours. Cell viability is measured using MTT or CCK-8 assays. Apoptosis is detected using Annexin V/PI staining, and cell cycle analysis is performed using flow cytometry. Autophagy is assessed by detecting LC3-II conversion and p62 degradation via Western blotting. Inflammatory responses are evaluated by measuring cytokine levels in the culture medium using ELISA.
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| Animal Protocol |
In vivo animal experiments for tubeimoside I are conducted using mouse models. For tumor growth studies, immunodeficient mice are subcutaneously implanted with cancer cells and then treated with tubeimoside I intraperitoneally or orally. Tumor size and weight are measured. In models of inflammation, such as LPS-induced acute lung injury, mice are treated with the compound before the LPS challenge, and lung tissues are analyzed for inflammatory cell infiltration and cytokine levels.
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| ADME/Pharmacokinetics |
Pharmacokinetic (PK) properties of tubeimoside I indicate it is orally active. The compound has a large molecular weight (1319.43) and is a triterpenoid saponin, which may affect its absorption and bioavailability. It is soluble in DMSO and is typically stored as a powder at -20°C. Detailed PK parameters, such as half-life and volume of distribution, are determined in animal studies via LC-MS/MS analysis of plasma samples.
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| Toxicity/Toxicokinetics |
Toxicology (toxicology) data for tubeimoside I are limited but suggest it is relatively safe at therapeutic doses. In animal studies, no significant decrease in body weight was observed in mice treated with the compound at doses up to 4 mg/kg intraperitoneally. However, as a saponin, it may cause hemolysis, and its safety profile requires thorough evaluation in long-term toxicology studies.
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| References |
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| Additional Infomation |
Other information: Tubeimoside I is a natural product derived from Bolbostemma paniculatum and is used as a research reagent. It has been studied for its potential in treating inflammatory diseases, various cancers, sepsis, and ischemic diseases. Its multi-targeting mechanism and ability to induce both apoptosis and autophagy make it a promising lead compound for drug development.
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| Molecular Formula |
C63H98O29
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|---|---|
| Molecular Weight |
1319.44
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| Exact Mass |
1318.619
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| CAS # |
102040-03-9
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| PubChem CID |
3034097
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| Appearance |
White to off-white solid powder
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| Density |
1.5±0.1 g/cm3
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| Index of Refraction |
1.637
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| LogP |
6.38
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| Hydrogen Bond Donor Count |
15
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| Hydrogen Bond Acceptor Count |
29
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| Rotatable Bond Count |
18
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| Heavy Atom Count |
92
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| Complexity |
2710
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| Defined Atom Stereocenter Count |
31
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| SMILES |
[C@@]12(CCC(C)(C)C[C@@]1([H])C1=CC[C@]3([H])[C@@]4(C)C[C@@H]([C@@H]5O[C@@H]6O[C@@H]([C@@H](O)[C@H](O)[C@H]6O[C@@H]6OC[C@H](O)[C@H](O)[C@H]6OC(=O)CC(O)(C)CC(=O)OC[C@@]5(C)[C@]4([H])CC[C@@]3(C)[C@]1(C)CC2)CO)O)C(=O)O[C@@H]1OC[C@H](O)[C@H](O)[C@H]1O[C@@H]1O[C@H]([C@H](O)[C@@H](O[C@@H]2OC[C@@H](O)[C@H](O)[C@H]2O)[C@H]1O)C
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| Synonyms |
Tubeimoside A; Tubeimoside-I; Tubeimoside I
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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 (~75.79 mM)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (1.89 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.5 mg/mL (1.89 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C,1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.5 mg/mL (1.89 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 0.7579 mL | 3.7895 mL | 7.5790 mL | |
| 5 mM | 0.1516 mL | 0.7579 mL | 1.5158 mL | |
| 10 mM | 0.0758 mL | 0.3789 mL | 0.7579 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.