Tilorone
- Product NameTilorone
- CAS27591-97-5
- CBNumberCB3875201
- MFC25H34N2O3
- MW410.55
- EINECS1806241-263-5
- MOL File27591-97-5.mol
Chemical Properties
| Boiling point: | 552.3±50.0 °C(Predicted) |
| Density | 1.102±0.06 g/cm3(Predicted) |
| pka | 9.67±0.25(Predicted) |
| form | Solid |
| color | Orange to red |
Tilorone Chemical Properties,Usage,Production
Uses
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[1][2][3][4][5].Definition
ChEBI: Tilorone is a member of the class of fluoren-9-ones that is 9H-fluoren-9-one which is substituted by a 2-(diethylamino)ethoxy group at positions 2 and 7. It is an interferon inducer and a selective alpha7 nicotinic acetylcholine receptor (alpha7 nAChR) agonist. Its hydrochloride salt is used as an antiviral drug. It has a role as an antiviral agent, an interferon inducer, an antineoplastic agent, an anti-inflammatory agent and a nicotinic acetylcholine receptor agonist. It is a member of fluoren-9-ones, a tertiary amino compound, an aromatic ether and a diether. It is a conjugate base of a tilorone(2+).in vivo
Tilorone (50-250 mg/kg; po; single dose) can induce a delayed but not prolonged interferon response; and affects circulating interferon levels in a dose-dependent manner[1].
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].
| Animal Model: | 6-week-old female mouse[1] |
| Dosage: | 250 mg/kg |
| Administration: | po; single dose |
| 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. |
| Animal Model: | Ebola virus disease (EVD) infected mouse model[2] |
| Dosage: | 25 mg/kg, 30 mg/kg, 50 mg/kg |
| Administration: | ip; once daily for 8 days |
| Result: | Showed was fully protective effect at 30 mg/kg, starting 2 or 24 h postchallenge and continuing through day 7 postinfection. |
| Animal Model: | C57BL/6 mouse[3] |
| Dosage: | 25 mg/kg |
| Administration: | IV; in 100μL saline via the lateral tail vein |
| Result: | Significant increased in the SUV mean of skeletal muscle, adipose tissue, and liver. |
References
[1] Stringfellow D A, et al. Tilorone hydrochloride: an oral interferon-inducing agent[J]. Antimicrobial agents and chemotherapy, 1972, 2(2): 73-78. DOI:10.1128/AAC.2.2.73[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. DOI:10.1128/AAC.01711-17
[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. DOI:10.1002/jcp.30998
[4] Wissing M D, et al. Small-molecule screening of PC3 prostate cancer cells identifies tilorone dihydrochloride to selectively inhibit cell growth based on cyclin-dependent kinase 5 expression[J]. Oncology reports, 2014, 32(1): 419-424.
Tilorone Supplier
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