Tilorone dihydrochloride
Based on 2 publication(s) in Google Scholar
Tilorone dihydrochloride is an orally active interferon (IFN) inducer with broad-spectrum antiviral activities. Tilorone dihydrochloride possesses robust anti-Severe fever with thrombocytopenia syndrome virus (SFTSV) activity in vitro and in vivo through stimulation of host innate immunity. Tilorone dihydrochloride can penetrate the blood-brain barrier to activate HIF in the CNS.Tilorone dihydrochloride exhibits an inhibitory activity with EC50 of 230 nM against Ebola virus (EBOV).
For research use only. We do not sell to patients.
- Purity: 99.29%
- CAS No.: 27591-69-1
- Formula: C25H36Cl2N2O3
- Molecular Weight:483.47
-
Storage:
4°C, sealed storage, away from moisture
* In solvent : -80°C, 1 year; -20°C, 6 months (sealed storage, away from moisture)
-
Biological Activity
-
Chemical Information
-
Solvent & Solubility
- Purity & Documentation
- References
-
Help & FAQs
-
Anti-Infection Compound Library
HY-L002
-
Epigenetics Compound Library
HY-L005
-
Immunology/Inflammation Compound Library
HY-L007
-
Metabolism/Protease Compound Library
HY-L012
-
FDA-Approved Drug Library
HY-L022
-
Antiviral Compound Library
HY-L027
-
CNS-Penetrant Compound Library
HY-L028
-
Drug Repurposing Compound Library
HY-L035
-
Reprogramming Compound Library
HY-L039
-
Oxygen Sensing Compound Library
HY-L045
-
Anti-COVID-19 Compound Library
HY-L052
-
Orally Active Compound Library
HY-L061
-
Glutamine Metabolism Compound Library
HY-L064
-
FDA Approved & Pharmacopeial Drug Library
HY-L066
-
Anti-Breast Cancer Compound Library
HY-L074
-
Anti-Cancer Metabolism Compound Library
HY-L083
-
Angiogenesis-Related Compound Library
HY-L088
-
Transcription Factor-Targeted Library
HY-L090
-
Rare Diseases Drug Library
HY-L102
-
Human Metabolite Library
HY-L123
-
Off-patent Drug Library
HY-L141
-
Metabolic Enzyme Compound Library
HY-L146
-
Anti-Hematopathy Compound Library
HY-L171
-
Multi-Target Compound Library
HY-L176
-
Bioactive Compound Library Max
HY-L181
-
MCE Bioactive Compound Library
HY-L001V
-
Drug Repurposing Compound Library Plus
HY-L035P
-
FDA-Approved Drug Library Plus
HY-L022P
-
FDA-Approved Drug Library Mini
HY-L022M
-
Bioactive Compound Library
HY-L001
-
Lactic Acid Metabolic Compound Library
HY-L204
-
High-Throughput Bioactive Compound Library
HY-L205
-
Mass Spectrometry Human Metabolite Library
HY-L215
Publications Citing Use of MedChemExpress (MCE) Tilorone dihydrochloride
More
Biological Activity
|
Cell Line
|
Type | Value | Description | References |
|---|---|---|---|---|
| A549 | IC50 |
32.63 μM
Compound: Tilorone hydrochloride
|
Anticancer activity against human A549 cells after 48 hrs by MTT assay
Anticancer activity against human A549 cells after 48 hrs by MTT assay
|
[PMID: 23665799] |
| HEK-293T | IC50 |
76.41 μM
Compound: Tilorone hydrochloride
|
Cytotoxicity against human HEK293T cells after 48 hrs by MTT assay
Cytotoxicity against human HEK293T cells after 48 hrs by MTT assay
|
[PMID: 23665799] |
| HeLa | IC50 |
39.97 μM
Compound: Tilorone hydrochloride
|
Anticancer activity against human HeLa cells after 48 hrs by MTT assay
Anticancer activity against human HeLa cells after 48 hrs by MTT assay
|
[PMID: 23665799] |
| Hep 3B2 | IC50 |
38.78 μM
Compound: Tilorone hydrochloride
|
Anticancer activity against human Hep3B cells after 48 hrs by MTT assay
Anticancer activity against human Hep3B cells after 48 hrs by MTT assay
|
[PMID: 23665799] |
| Vero | IC50 |
89.53 μM
Compound: Tilorone hydrochloride
|
Cytotoxicity against African green monkey Vero cells after 48 hrs by MTT assay
Cytotoxicity against African green monkey Vero cells after 48 hrs by MTT assay
|
[PMID: 23665799] |
Tilorone (0.1, 0.3, 1 μM) dihydrochloride inhibits SFTSV-induced cytopathological effect (CPE) in a dose-dependent manner with no cell toxicity in Huh7 cells[1].
Tilorone dihydrochloride reveals drug-like properties, with solubility of 465 μM at pH 7.4, stable mouse microsomal metabolity (half-time: 47.8 min; CL: 14.5 μL/min/mg) and Caco-2 permeability (10 μM) of 20.4×10-6 cm/s and 8.87×10-6 cm/s[4].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Tilorone (5, 10 mg/kg; intraperitoneally; 12 h prior to challenge, at the time point of challenge, and 12 h after challenge) dihydrochloride with 10 mg/kg dose-dependently inhibits viremia, causes a general increase in IFN-α and IFN-β, reduces the TNF-α and IL-10 in a viremia model based on wild-type 6-week-old female BALB/c mice with SFTSV[1].
Tilorone dihydrochloride (10-50 mg/kg, i.p., once daily for 8 days) exhibits a dose-efficient range against EBOV of 25-50 mg/kg, with full clearance of virus in mice[4].
Tilorone dihydrochloride (30-60 mg/kg, i.p., once, 2 h , 24 h and 48 h postinfection) reveals 100% survival rate at dosage of 30 mg/kg in BALB/c mice, when dosed at 2 h and 24 h postinfection[4]. Tilorone dihydrochloride (2-10 mg/kg, once, i.p.) reveals a pharmacokinetic parameter in BLAB/c mice [4]:
Pharmacokinetic Analysis of Tilorone in BALB/c mice[1]
| Dose (mg/kg) | Sex | T1/2 (h) | Tmax (h) | Cmax (ng/ml) | AUClast (ng·h/ml) | AUCinf (ng·h/ml) | CLblood (ml/h/kg) | V (ml/kg) |
| 2 | M | 15.7 | 0.083 | 50.5 | 356 | 516 | 87900 | 3870 |
| 2 | F | 18.7 | 0.083 | 17.5 | 133 | 210 | 257000 | 9510 |
| 10 | M | 20.8 | 0.25 | 135 | 1099 | 1940 | 155000 | 5160 |
| 10 | F | 18.9 | 0.25 | 92.3 | 513 | 793 | 343000 | 12600 |
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
-
Animal Model:Wild-type 1-day-old suckling ICR mice with ethal virus challenge model[1]
-
Dosage:5, 10, 20 mg/kg
-
Administration:Intraperitoneally; once daily at 1-7 days
-
Result:Protected 78.94% of the mice from lethal challenge, compared with none in the vehicle group at 21 days post infection.
-
Animal Model:EBOV in BLAB/c mice[4]
-
Dosage:30-60 mg/kg
-
Administration:Intraperitoneal injection, signle dosage: 2 h, 24 h and 48 h postinfection
-
Result:Exhibited 100% survival rates at 2 h and 24 h postinfection, with dosage of 30 mg/kg.
Chemical Information
-
CAS No. 27591-69-1
-
Appearance Solid
-
Molecular Weight 483.47
-
Formula C25H36Cl2N2O3
-
Color Light yellow to orange
-
SMILES
O=C1C2=C(C3=C1C=C(OCCN(CC)CC)C=C3)C=CC(OCCN(CC)CC)=C2.[H]Cl.[H]Cl
-
Shipping
Room temperature in continental US; may vary elsewhere.
-
Storage
4°C, sealed storage, away from moisture
* In solvent : -80°C, 1 year; -20°C, 6 months (sealed storage, away from moisture)
Publications (2)
-
Journal Impact Factor
-
Most Recent
-
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 -
Biomed J
2020 Aug;43(4):368-374. PMID: 32563698
Solvent & Solubility
H2O : 100 mg/mL (206.84 mM; Need ultrasonic)
DMSO : 12.5 mg/mL (25.85 mM; Need ultrasonic; 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, 1 year; -20°C, 6 months (sealed storage, away from moisture). When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
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, 1 year; -20°C, 6 months (sealed storage, away from moisture). When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
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: ≥ 1.25 mg/mL (2.59 mM); Clear solution
This protocol yields a clear solution of ≥ 1.25 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (12.5 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: ≥ 1.25 mg/mL (2.59 mM); Clear solution
This protocol yields a clear solution of ≥ 1.25 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (12.5 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.
For the following dissolution methods, please prepare the working solution directly:
It is recommended to prepare fresh solutions and use them promptly within a short period of time.
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: PBS
Solubility: 25 mg/mL (51.71 mM); Clear solution; Need ultrasonic
Please enter the basic information of animal experiments:
-
-
-
-
Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Working solution concentration: 0.22 mg/mL
This product has good water solubility, please refer to the measured solubility data in water/PBS/Saline for details.
Purity & Documentation
-
Data Sheet (278 KB)
-
SDS (419 KB)
- English - EN (419 KB)
- Français - FR (419 KB)
- Deutsch - DE (419 KB)
- Norwegian - NO (419 KB)
- Español - ES (419 KB)
- Swedish - SV (419 KB)
- Italian - IT (419 KB)
- Korean - KR (419 KB)
- Portuguese - PT (419 KB)
-
Handling Instructions (2659 KB)
References
[1]. Jingjing Yang, et al. Tilorone confers robust in vitro and in vivo antiviral effects against severe fever with thrombocytopenia syndrome virus. Virol Sin. 2022 Feb;37(1):145-148. [Content Brief]
[2]. Sean Ekins, et al. Tilorone, a Broad-Spectrum Antiviral for Emerging Viruses. Antimicrob Agents Chemother. 2020 Apr 21;64(5):e00440-20. [Content Brief]
[3]. Rajiv R Ratan, et al. Small molecule activation of adaptive gene expression: tilorone or its analogs are novel potent activators of hypoxia inducible factor-1 that provide prophylaxis against stroke and spinal cord injury. Ann N Y Acad Sci. 2008 Dec:1147:383-94. [Content Brief]
[4]. Ekins S, et al., Efficacy of Tilorone Dihydrochloride against Ebola Virus Infection. Antimicrob Agents Chemother. 2018 Jan 25;62(2):e01711-17. [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, 1 year; -20°C, 6 months (sealed storage, away from moisture). When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO / H2O | 1 mM | 2.0684 mL | 10.3419 mL | 20.6838 mL | 51.7095 mL |
| 5 mM | 0.4137 mL | 2.0684 mL | 4.1368 mL | 10.3419 mL | |
| 10 mM | 0.2068 mL | 1.0342 mL | 2.0684 mL | 5.1710 mL | |
| 15 mM | 0.1379 mL | 0.6895 mL | 1.3789 mL | 3.4473 mL | |
| 20 mM | 0.1034 mL | 0.5171 mL | 1.0342 mL | 2.5855 mL | |
| 25 mM | 0.0827 mL | 0.4137 mL | 0.8274 mL | 2.0684 mL | |
| H2O | 30 mM | 0.0689 mL | 0.3447 mL | 0.6895 mL | 1.7237 mL |
| 40 mM | 0.0517 mL | 0.2585 mL | 0.5171 mL | 1.2927 mL | |
| 50 mM | 0.0414 mL | 0.2068 mL | 0.4137 mL | 1.0342 mL | |
| 60 mM | 0.0345 mL | 0.1724 mL | 0.3447 mL | 0.8618 mL | |
| 80 mM | 0.0259 mL | 0.1293 mL | 0.2585 mL | 0.6464 mL | |
| 100 mM | 0.0207 mL | 0.1034 mL | 0.2068 mL | 0.5171 mL |
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
Powered by Bioz