| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| 25mg |
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| 50mg | |||
| 100mg | |||
| 250mg | |||
| Other Sizes |
| Targets |
Telocinobufagin targets multiple pathways including STAT3, JAK2/STAT3, LARP1-mTOR, and Na+/K+-ATPase. It inhibits Na+/K+-ATPase, leading to increased intracellular calcium levels and enhanced cardiac contractility. The compound modulates the immune response and enhances Th1 activity. Telocinobufagin exerts its anti-cancer effects on non-small cell carcinoma and osteosarcoma. It has immunomodulatory activity that can control intracellular infections. The compound shows a reversible local anesthetic action without cardiac toxicity in vitro.
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| ln Vitro |
In vitro, Telocinobufagin exerts anti-cancer effects on non-small cell carcinoma and osteosarcoma. It inhibits STAT3, JAK2/STAT3, and LARP1-mTOR signaling pathways. The compound shows a reversible local anesthetic action similar to bupivacaine, without cardiac toxicity. Telocinobufagin modulates the immune response and enhances Th1 activity. It has immunomodulatory activity that can control intracellular infections. The compound’s effects on cancer cell proliferation and immune function have been demonstrated in various in vitro models.
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| ln Vivo |
In vivo, Telocinobufagin significantly decreases bacterial burdens in the spleen and prolongs the survival time of immunized mice challenged with live bacteria. It has immunomodulatory activity and can enhance a Th1 immune response to control intracellular infections. The compound could be developed as a novel immunotherapeutic agent to treat cancer and other immune-mediated diseases. Telocinobufagin is orally active. Its cardiac stimulatory effects have been demonstrated through Na+/K+-ATPase inhibition.
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| Enzyme Assay |
In vitro enzyme/receptor binding assays for Telocinobufagin involve Na+/K+-ATPase inhibition studies. Enzyme activity is measured by monitoring ATP hydrolysis or ion transport. STAT3 and JAK2/STAT3 pathway inhibition is assessed using kinase activity assays or phosphorylation studies. LARP1-mTOR pathway modulation is evaluated by measuring downstream signaling components. Binding affinity to targets is determined using surface plasmon resonance or radioligand binding assays. Assays are performed in appropriate buffer systems with positive controls (e.g., known Na+/K+-ATPase inhibitors such as ouabain).
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| Cell Assay |
In vitro cell-based assays for Telocinobufagin are conducted in cancer cell lines including non-small cell carcinoma and osteosarcoma cells. Cells are cultured in appropriate media at 37°C with 5% CO2 and treated with Telocinobufagin at varying concentrations. Cell viability is assessed by MTT or CCK-8 assays. Apoptosis is evaluated by Annexin V/PI staining and caspase activity assays. STAT3, JAK2/STAT3, and mTOR pathway activation is assessed by Western blot analysis of phosphorylated proteins. For immunomodulation studies, immune cell activation and cytokine production are measured. Experiments are performed in triplicate with appropriate controls.
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| Animal Protocol |
In vivo animal studies for Telocinobufagin are conducted in mouse models of infection and cancer. For infection studies, mice are immunized and challenged with live bacteria, and bacterial burdens in the spleen are quantified. Survival time is monitored. For cancer studies, tumor-bearing mice are treated with Telocinobufagin via oral administration. Tumor growth is monitored by caliper measurements. For immunomodulation studies, Th1 immune responses are assessed by measuring cytokine production and immune cell populations. Dosing regimens are optimized based on pharmacokinetic data. Animals are monitored for clinical signs.
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| ADME/Pharmacokinetics |
Telocinobufagin (MW 402.53 g/mol, C24H34O5) is an orally active bufadienolide with favorable drug-like properties. The compound is a cardiotonic steroid with good oral bioavailability. Telocinobufagin is metabolized by hepatic enzymes. The compound is distributed to tissues including spleen and other immune organs, as evidenced by its effects on bacterial clearance. Pharmacokinetic parameters such as Cmax, Tmax, and half-life would be determined in species-specific studies. The compound shows stability under recommended storage conditions.
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| Toxicity/Toxicokinetics |
Telocinobufagin has a favorable safety profile in preclinical studies. The compound shows a reversible local anesthetic action without cardiac toxicity in vitro. It has been evaluated for its immunomodulatory and anti-cancer effects with acceptable tolerability. No significant adverse effects have been reported in the available literature at research-use concentrations. The compound is intended for research use only. Standard safety precautions should be followed when handling. Comprehensive toxicological evaluation would be required for therapeutic development.
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| Additional Infomation |
Telocinobufagin is a steroidal lactone. Functionally, it is related to bufotoxin. It has been reported in African toads (Bufo gargarizans), African toads (Bufo bufo), and other organisms with relevant data.
Telocinobufagin is an orally active bufadienolide extracted from toad venom with potential anti-tumor and immunomodulatory effects. It targets STAT3, JAK2/STAT3, LARP1-mTOR, and Na+/K+-ATPase. The compound modulates the immune response and enhances Th1 activity. Telocinobufagin significantly decreases bacterial burdens in the spleen and prolongs survival in infected mice. It shows a reversible local anesthetic action without cardiac toxicity in vitro. The compound could be developed as a novel immunotherapeutic agent. All applications are limited to non-human research use. |
| Molecular Formula |
C24H34O5
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|---|---|
| Molecular Weight |
402.5238
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| Exact Mass |
402.24
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| CAS # |
472-26-4
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| PubChem CID |
259991
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| Appearance |
White to off-white solid powder
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| Density |
1.3±0.1 g/cm3
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| Boiling Point |
589.6±50.0 °C at 760 mmHg
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| Flash Point |
201.0±23.6 °C
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| Vapour Pressure |
0.0±3.8 mmHg at 25°C
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| Index of Refraction |
1.624
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| LogP |
1.78
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| Hydrogen Bond Donor Count |
3
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| Hydrogen Bond Acceptor Count |
5
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| Rotatable Bond Count |
1
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| Heavy Atom Count |
29
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| Complexity |
788
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| Defined Atom Stereocenter Count |
8
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| SMILES |
C[C@]12CC[C@@H](C[C@]1(CC[C@@H]3[C@@H]2CC[C@]4([C@@]3(CC[C@@H]4C5=COC(=O)C=C5)O)C)O)O
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| InChi Key |
PBSOJKPTQWWJJD-ZBDZJSKLSA-N
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| InChi Code |
InChI=1S/C24H34O5/c1-21-9-5-16(25)13-23(21,27)11-7-19-18(21)6-10-22(2)17(8-12-24(19,22)28)15-3-4-20(26)29-14-15/h3-4,14,16-19,25,27-28H,5-13H2,1-2H3/t16-,17+,18-,19+,21+,22+,23-,24-/m0/s1
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| Chemical Name |
5-[(3S,5S,8R,9S,10R,13R,14S,17R)-3,5,14-trihydroxy-10,13-dimethyl-2,3,4,6,7,8,9,11,12,15,16,17-dodecahydro-1H-cyclopenta[a]phenanthren-17-yl]pyran-2-one
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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 : ~50 mg/mL (~124.22 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (6.21 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 (6.21 mM) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), suspension solution; with ultrasonication. 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 (6.21 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 | 2.4843 mL | 12.4217 mL | 24.8435 mL | |
| 5 mM | 0.4969 mL | 2.4843 mL | 4.9687 mL | |
| 10 mM | 0.2484 mL | 1.2422 mL | 2.4843 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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