| Size | Price | Stock | Qty |
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| 5mg |
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| Other Sizes |
| Targets |
Resibufagin's primary mechanism of action involves the inhibition of Na⁺/K⁺-ATPase, a key membrane-bound enzyme that maintains electrochemical gradients across cell membranes. Bufadienolides are known to bind to the extracellular domain of the Na⁺/K⁺-ATPase α-subunit, inhibiting its activity and leading to increased intracellular sodium and calcium concentrations. This disruption of ion homeostasis triggers downstream signaling cascades, including the activation of various kinases and apoptotic pathways. Molecular docking studies have suggested potential interactions with targets such as EGFR and PIK3CA. The compound's cytotoxic activity against cancer cells is attributed to the induction of apoptosis through these signaling pathways.
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| ln Vitro |
Resibufagin shows strong cytotoxic activity against the HeLa cell line, a human cervical cancer cell line. In vitro studies have demonstrated that resibufagin and related bufadienolides exhibit potent antiproliferative effects against various cancer cell lines. The compound's cytotoxicity is attributed to its ability to inhibit Na⁺/K⁺-ATPase, leading to disrupted ion homeostasis, increased intracellular calcium, and activation of apoptotic signaling pathways. Structure-activity relationship studies of bufadienolides indicate that the presence of specific functional groups, including hydroxyl and acetoxy substitutions, significantly influences their cytotoxic potency.
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| ln Vivo |
In vivo studies of resibufagin are limited, as most research has focused on its in vitro cytotoxic activity. As a bufadienolide isolated from Chan'Su, it is expected to contribute to the pharmacological effects of toad venom, which has been used in traditional Chinese medicine for its antitumor, cardiotonic, and analgesic properties. Bufadienolides are known to have potent cardiotonic effects in vivo due to their inhibition of Na⁺/K⁺-ATPase, which can increase cardiac contractility. However, this also contributes to their narrow therapeutic index and potential cardiotoxicity. Further in vivo studies are needed to fully characterize the pharmacokinetic and pharmacodynamic properties of resibufagin.
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| Enzyme Assay |
Non-cell-based assays for resibufagin typically involve Na⁺/K⁺-ATPase inhibition assays using purified enzyme preparations. The enzyme is incubated with ATP and the substrate p-nitrophenyl phosphate, and the release of p-nitrophenol is measured spectrophotometrically at 405 nm. Various concentrations of resibufagin are tested to determine the IC₅₀ value for enzyme inhibition. Molecular docking studies can be performed using crystal structures of Na⁺/K⁺-ATPase to predict binding modes and affinity. For compound characterization, standard analytical methods including HPLC, NMR, and mass spectrometry are used to confirm identity and purity.
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| Cell Assay |
Cell-based assays for resibufagin are primarily cytotoxicity studies using cancer cell lines such as HeLa (cervical cancer), as well as other lines including MCF-7 (breast cancer), A549 (lung cancer), and HepG2 (liver cancer). Cells are cultured in appropriate medium and treated with resibufagin at various concentrations (typically 0.1-100 μM) for 24-72 hours. Cell viability is assessed using MTT, CCK-8, or SRB assays. Apoptosis is evaluated by flow cytometry using Annexin V/PI staining, caspase activity assays, and detection of apoptotic markers by Western blot. Cell cycle analysis is performed by propidium iodide staining and flow cytometry.
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| Animal Protocol |
In vivo studies of resibufagin are limited in the published literature. Based on related bufadienolides, potential animal models include: mouse xenograft models bearing human cancer cell lines for antitumor evaluation; and cardiotonic activity assessment in animal models of heart failure. Standard protocols for xenograft studies involve subcutaneous implantation of cancer cells in immunodeficient mice, followed by administration of the compound (typically intraperitoneal or intravenous) when tumors reach a certain size. Tumor volume is measured over time, and tissues are collected for histopathological and biomarker analysis.
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| ADME/Pharmacokinetics |
Pharmacokinetic data for resibufagin are limited. As a bufadienolide with a molecular weight of 398.50 g/mol and a molecular formula of C₂₄H₃₀O₅, it is expected to have moderate lipophilicity and oral bioavailability. Bufadienolides are generally characterized by poor oral bioavailability due to extensive first-pass metabolism and are often administered parenterally. The compound has a relative density of 1.31 g/cm³. It should be stored as a powder at -20°C for up to 3 years or in solvent at -80°C for 1 year. The compound is typically soluble in organic solvents such as DMSO and ethanol.
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| Toxicity/Toxicokinetics |
Specific toxicity data for resibufagin are limited. Bufadienolides as a class are known to have a narrow therapeutic index due to their potent inhibition of Na⁺/K⁺-ATPase, which can lead to cardiotoxicity at high doses. Cardiotoxic effects include arrhythmias, increased contractility, and potentially fatal cardiac arrest. The compound exhibits strong cytotoxic activity against cancer cell lines, indicating significant biological activity at low concentrations. Standard laboratory safety practices should be followed when handling this compound, including the use of personal protective equipment. It is intended for research use only and is not for human consumption.
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| References | |
| Additional Infomation |
Resibufagin is a bufadienolide isolated from the traditional Chinese medicine Chan'Su (toad venom from Bufo bufo gargarizans). Chan'Su has been used in traditional Chinese medicine for its cardiotonic, analgesic, and antitumor properties. Resibufagin, along with other bufadienolides such as bufalin, cinobufagin, and resibufogenin, contributes to the pharmacological activities of toad venom. The compound's strong cytotoxic activity against HeLa cells makes it of interest for anticancer research. It is used as a reference standard for quality control of Chan'Su preparations and for research purposes. The compound is for research use only.
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| Molecular Formula |
C24H30O5
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| Molecular Weight |
398.49
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| Exact Mass |
398.209
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| CAS # |
20987-24-0
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| PubChem CID |
11969466
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| Appearance |
White to light yellow solid powder
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| Density |
1.3±0.1 g/cm3
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| Boiling Point |
592.1±50.0 °C at 760 mmHg
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| Flash Point |
205.2±23.6 °C
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| Vapour Pressure |
0.0±3.8 mmHg at 25°C
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| Index of Refraction |
1.613
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| LogP |
1.43
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
5
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| Rotatable Bond Count |
2
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| Heavy Atom Count |
29
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| Complexity |
831
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| Defined Atom Stereocenter Count |
8
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| SMILES |
C[C@]12CC[C@H]3[C@H]([C@@]14[C@H](O4)CC2C5=COC(=O)C=C5)CC[C@H]6[C@@]3(CC[C@@H](C6)O)C=O
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| InChi Key |
LFLJTMIVTFTLOA-UIZOPSFESA-N
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| InChi Code |
InChI=1S/C24H30O5/c1-22-8-7-17-18(4-3-15-10-16(26)6-9-23(15,17)13-25)24(22)20(29-24)11-19(22)14-2-5-21(27)28-12-14/h2,5,12-13,15-20,26H,3-4,6-11H2,1H3/t15-,16+,17+,18-,19?,20-,22-,23-,24-/m1/s1
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| Chemical Name |
(1R,2S,4R,7R,10S,11R,14S,16R)-14-hydroxy-7-methyl-6-(6-oxopyran-3-yl)-3-oxapentacyclo[8.8.0.02,4.02,7.011,16]octadecane-11-carbaldehyde
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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 and light. |
| 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: ≥ 50 mg/mL (125.47 mM)
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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 | 2.5095 mL | 12.5474 mL | 25.0947 mL | |
| 5 mM | 0.5019 mL | 2.5095 mL | 5.0189 mL | |
| 10 mM | 0.2509 mL | 1.2547 mL | 2.5095 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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