| Size | Price | Stock | Qty |
|---|---|---|---|
| 250mg |
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| 500mg |
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| 1g |
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| 2g | |||
| Other Sizes |
Purity: ≥98%
| Targets |
Tilorone dihydrochloride acts as an interferon (IFN) inducer, stimulating the host innate immune system. It activates interferon production through the IFNAR pathway. It also has antineoplastic and anti-inflammatory actions. It has been shown to be a DNA intercalator. It is a nicotinic acetylcholine receptor agonist. Its broad-spectrum antiviral activity is mediated through stimulation of host innate immunity.
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| ln Vitro |
Tilorone dihydrochloride is an orally active interferon inducer with broad-spectrum antiviral activities. It possesses robust anti-Severe fever with thrombocytopenia syndrome virus (SFTSV) activity in vitro and in vivo. It exhibits both antineoplastic and anti-inflammatory actions. It has been used to treat influenza, herpesvirus infections, viral hepatitis, and acute respiratory viral infections.
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| ln Vivo |
In vivo, Tilorone dihydrochloride has been shown to have broad-spectrum antiviral activity, including against SFTSV, through stimulation of host innate immunity. It has been used as an antiviral drug in Russia for the treatment of influenza, herpesvirus infections, viral hepatitis, and acute respiratory viral infections. It also has antitumor and anti-inflammatory properties.
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| Enzyme Assay |
In vitro enzyme assays for Tilorone dihydrochloride are not typical, as its mechanism involves interferon induction and immune modulation. However, its effects on interferon production can be measured in cell-based assays. Its DNA intercalation activity can be studied using biochemical assays such as gel electrophoresis or fluorescence spectroscopy.
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| Cell Assay |
In vitro cellular assays for Tilorone dihydrochloride involve treating cells with the compound and measuring interferon production by ELISA or bioassay. Its antiviral activity is assessed by measuring viral replication in infected cell cultures. Its anti-inflammatory effects are evaluated by measuring cytokine production in stimulated immune cells. Its cytotoxicity is measured using MTT or similar assays.
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| Animal Protocol |
In vivo animal models for Tilorone dihydrochloride include models of viral infection to evaluate its antiviral efficacy. Mice are infected with a virus and treated with the compound, and survival or viral load is measured. Its anti-inflammatory and antitumor effects are studied in appropriate models. Its ability to induce interferon production is measured in serum.
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| ADME/Pharmacokinetics |
Tilorone dihydrochloride is orally active. It is well-absorbed after oral administration and can cross the blood-brain barrier. It is metabolized in the liver, and its metabolites are excreted in urine and feces. Its half-life and bioavailability are consistent with its use as an antiviral drug. Its pharmacokinetics have been characterized in preclinical and clinical studies.
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| Toxicity/Toxicokinetics |
Tilorone dihydrochloride is generally well-tolerated. Common side effects may include gastrointestinal disturbances, headache, and dizziness. As an interferon inducer, it may cause flu-like symptoms. Its safety has been evaluated in clinical studies in Russia. It has shown a favorable safety profile for the treatment of viral infections.
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| References |
Ekins S, Lingerfelt MA, Comer JE, Freiberg AN, Mirsalis JC, O'Loughlin K, Harutyunyan A, McFarlane C, Green CE, Madrid PB. Efficacy of Tilorone Dihydrochloride against Ebola Virus Infection. Antimicrob Agents Chemother. 2017 Nov 13. pii: AAC.01711-17. doi: 10.1128/AAC.01711-17. [Epub ahead of print] PubMed PMID: 29133569.
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| Additional Infomation |
Telodeon dihydrochloride is the dihydrochloride salt of tinoxone. It is an antiviral drug used to treat influenza, herpesvirus infections, viral hepatitis, acute respiratory viral infections, and SARS. It has multiple effects, including anti-inflammatory, antitumor, interferon-inducing, nicotinic acetylcholine receptor agonist, and antiviral activity. It contains tinoxone (2+) ions. It is an antiviral drug used in its hydrochloride form. It is the first approved synthetic low molecular weight orally active interferon inducer and has also been reported to have antitumor and anti-inflammatory effects.
Tilorone dihydrochloride is an orally active, synthetic interferon inducer with broad-spectrum antiviral activities. It is a fluorenone derivative and the first recognized synthetic oral interferon inducer. It has been used as an antiviral drug in Russia. It also has antitumor, anti-inflammatory, and nicotinic acetylcholine receptor agonist properties. It crosses the blood-brain barrier. |
| Molecular Formula |
C25H36CL2N2O3
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|---|---|
| Molecular Weight |
483.474
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| Exact Mass |
482.21
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| CAS # |
27591-69-1
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| Related CAS # |
27591-69-1;
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| PubChem CID |
33958
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| Appearance |
Light yellow to orange solid powder
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| Density |
1.102g/cm3
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| Boiling Point |
552.3ºC at 760 mmHg
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| Melting Point |
230-233 °C(lit.)
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| Flash Point |
287.8ºC
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| Vapour Pressure |
3.05E-12mmHg at 25°C
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| LogP |
5.943
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| Hydrogen Bond Donor Count |
2
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| Hydrogen Bond Acceptor Count |
5
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| Rotatable Bond Count |
12
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| Heavy Atom Count |
32
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| Complexity |
477
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| Defined Atom Stereocenter Count |
0
|
| SMILES |
Cl[H].Cl[H].O(C([H])([H])C([H])([H])N(C([H])([H])C([H])([H])[H])C([H])([H])C([H])([H])[H])C1C([H])=C([H])C2=C(C=1[H])C(C1C([H])=C(C([H])=C([H])C2=1)OC([H])([H])C([H])([H])N(C([H])([H])C([H])([H])[H])C([H])([H])C([H])([H])[H])=O
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| InChi Key |
BSVYJQAWONIOOU-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C25H34N2O3.2ClH/c1-5-26(6-2)13-15-29-19-9-11-21-22-12-10-20(30-16-14-27(7-3)8-4)18-24(22)25(28)23(21)17-19/h9-12,17-18H,5-8,13-16H2,1-4H32*1H
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| Chemical Name |
2,7-Bis[2-(diethylamino)ethoxy]fluoren-9-one dihydrochloride
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| Synonyms |
Tilorone dihydrochloride
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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, 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 (~206.84 mM)
DMSO : ~12.5 mg/mL (~25.85 mM) |
|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 1.25 mg/mL (2.59 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 12.5 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: ≥ 1.25 mg/mL (2.59 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 12.5 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: 25 mg/mL (51.71 mM) in PBS (add these co-solvents sequentially from left to right, and one by one), clear solution; with ultrasonication. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.0684 mL | 10.3419 mL | 20.6838 mL | |
| 5 mM | 0.4137 mL | 2.0684 mL | 4.1368 mL | |
| 10 mM | 0.2068 mL | 1.0342 mL | 2.0684 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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