Tilorone
Based on 2 publication(s) in Google Scholar
Tilorone is an orally active antiviral agent and interferon inducer that also has potential antineoplastic, immunomodulatory, and metabolic modulating effects. Tilorone induces an abnormally delayed interferon response and primarily stimulates interferon production in lymphoid tissue. Thus, Tilorone exerts antiviral effects and can be used as a chemotherapeutic agent. Tilorone has the potential to inhibit type 2 diabetes by increasing glucose uptake in vivo and in skeletal muscle cells by enhancing Akt2/AS160 signaling and glucose transporter levels.
For research use only. We do not sell to patients.
- Purity: 99.80%
- CAS No.: 27591-97-5
- Formula: C25H34N2O3
- Molecular Weight:410.55
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Storage:
-20°C, protect from light
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
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Biological Activity
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Chemical Information
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Solvent & Solubility
- Purity & Documentation
- References
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Help & FAQs
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Publications Citing Use of MedChemExpress (MCE) Tilorone
More
Biological Activity
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| HeLa | IC50 |
1.14 μM
Compound: Tilorone
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Antiviral activity against Ebolavirus infected in human HeLa cells assessed as reduction in viral replication incubated for 48 hrs by luminescence based assay
Antiviral activity against Ebolavirus infected in human HeLa cells assessed as reduction in viral replication incubated for 48 hrs by luminescence based assay
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[PMID: 32832035] |
| Oocyte | EC50 |
2.5 μM
Compound: 1
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Agonist activity at human recombinant alpha7 nAChR expressed in xenopus oocytes by patch clamp assay
Agonist activity at human recombinant alpha7 nAChR expressed in xenopus oocytes by patch clamp assay
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[PMID: 22281189] |
| Vero | CC50 |
19.67 μM
Compound: Tilorone
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Cell viability measured by CellTiter-Glo assay in Vero cells at MOI 0.05 after 72hr
Cell viability measured by CellTiter-Glo assay in Vero cells at MOI 0.05 after 72hr
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10.1101/2020.03.20.999730 |
| Vero | IC50 |
4.09 μM
Compound: Tilorone
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Antiviral activity against SARS-CoV-2 (viral titer) measured by plaque assay in Vero cells at MOI 0.0125 after 24 hr
Antiviral activity against SARS-CoV-2 (viral titer) measured by plaque assay in Vero cells at MOI 0.0125 after 24 hr
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10.1101/2020.03.20.999730 |
Tilorone (0.8-500 μg/mL; 2 d) induces insignificant interferon production in peritoneal macrophages and lymphocytes[1].
Tilorone has 52% of human plasma proteins Binding rate, excellent plasma stability, mouse liver microsomal half-life of 48 minutes[2].
Tilorone (20, 35 nM; 40 h) increases bone morphology in myoblasts The expression of BMP and Smad4[3].
Tilorone (20, 35 nM; 40 h) can also increase the expression of GLUT and glucose uptake in C2C12 cells[3] .
Tilorone (3 μM-20 μM; 72 h) can also selectively target PC3 cells with low CDK5 activity[4] .
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:Myoblasts
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Concentration:20 nM, 35 nM
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Incubation Time:40 h
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Result:Increased the phosphorylation of Smad1/5/8, indicating the enhancement of BMP signaling.
The maximum tolerated single dose of Tilorone in mice is 100 mg/kg; pharmacokinetic results of Tilorone (2, 10 mg/kg; ip) in mice indicate that Tilorone has a high absorption rate and is The half-life in mice is 18 hours, but exposure in male mice is higher[2].
Tilorone (25-50 mg/kg; ip; once daily for 8 days ) protects 90% of Ebola virus-infected mice from lethal challenge[2].
Tilorone (25 mg/kg; iv; single dose) enhances immunity in small Uptake of the radiolabeled glucose analog 18F-fluoro-2-deoxyglucose in rats[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:6-week-old female mouse[1]
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Dosage:250 mg/kg
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Administration:po; single dose
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Result:Resulted in correspondingly lower levels of circulating interferon, although moderately high levels were obtained (2,500 units/ml) with as little as 50 mg/kg. Interferon production was not detected in the upper gastrointestinal tract.
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Animal Model:Ebola virus disease (EVD) infected mouse model[2]
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Dosage:25 mg/kg, 30 mg/kg, 50 mg/kg
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Administration:ip; once daily for 8 days
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Result:Showed was fully protective effect at 30 mg/kg, starting 2 or 24 h postchallenge and continuing through day 7 postinfection.
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Animal Model:C57BL/6 mouse[3]
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Dosage:25 mg/kg
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Administration:IV; in 100 μL saline via the lateral tail vein
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Result:Significant increased in the SUV mean of skeletal muscle, adipose tissue, and liver.
Chemical Information
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CAS No. 27591-97-5
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Appearance Solid
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Molecular Weight 410.55
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Formula C25H34N2O3
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Color Orange to red
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SMILES
O=C1C2=C(C3=C1C=C(OCCN(CC)CC)C=C3)C=CC(OCCN(CC)CC)=C2
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
-20°C, protect from light
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
Publications (2)
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Journal Impact Factor
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Most Recent
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Biomed J
2020 Aug;43(4):368-374. PMID: 32563698 -
Bioorg Chem
Identification of FTY720 and COH29 as novel topoisomerase I catalytic inhibitors by experimental and computational studies. [Abstract]2024 Jun:147:107412. PMID: 38696845
Solvent & Solubility
DMSO : 25 mg/mL (60.89 mM; ultrasonic and warming and heat to 60°C; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (protect from light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (protect from light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (6.09 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.5 mg/mL (6.09 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL. * In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Purity & Documentation
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Data Sheet (276 KB)
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SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
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Handling Instructions (2659 KB)
References
[1]. Stringfellow D A, et al. Tilorone hydrochloride: an oral interferon-inducing agent[J]. Antimicrobial agents and chemotherapy, 1972, 2(2): 73-78. [Content Brief]
[2]. Ekins S, et al. Efficacy of tilorone dihydrochloride against Ebola virus infection[J]. Antimicrobial agents and chemotherapy, 2018, 62(2): 10.1128/aac. 01711-17. [Content Brief]
[3]. Kohler Z M, et al. Tilorone increases glucose uptake in vivo and in skeletal muscle cells by enhancing Akt2/AS160 signaling and glucose transporter levels[J]. Journal of Cellular Physiology, 2023, 238(5): 1080-1094. [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (protect from light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 2.4358 mL | 12.1788 mL | 24.3576 mL | 60.8939 mL |
| 5 mM | 0.4872 mL | 2.4358 mL | 4.8715 mL | 12.1788 mL | |
| 10 mM | 0.2436 mL | 1.2179 mL | 2.4358 mL | 6.0894 mL | |
| 15 mM | 0.1624 mL | 0.8119 mL | 1.6238 mL | 4.0596 mL | |
| 20 mM | 0.1218 mL | 0.6089 mL | 1.2179 mL | 3.0447 mL | |
| 25 mM | 0.0974 mL | 0.4872 mL | 0.9743 mL | 2.4358 mL | |
| 30 mM | 0.0812 mL | 0.4060 mL | 0.8119 mL | 2.0298 mL | |
| 40 mM | 0.0609 mL | 0.3045 mL | 0.6089 mL | 1.5223 mL | |
| 50 mM | 0.0487 mL | 0.2436 mL | 0.4872 mL | 1.2179 mL | |
| 60 mM | 0.0406 mL | 0.2030 mL | 0.4060 mL | 1.0149 mL |
Tilorone Related Classifications
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