Cat. No.: HY-B1080A

Tilorone

2 Cited Publications

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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.

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Pureté: 99.80%
CAS No.: 27591-97-5
Formule: C₂₅H₃₄N₂O₃
Masse moléculaire:410.55

Stockage:

-20°C, protect from light

* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

Tilorone Chemical Structure

CAS No.: 27591-97-5

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Activité biologique
- Description
- Cellular Effect
- In Vitro
- In Vivo
Chemical Information
Publications (2)
Solvant et solubilité
- In Vitro
- In Vivo
Pureté et documentation
Références
Help & FAQs
Classifications
Bioz

Activité biologique

Description

Voir tous les produits spécifiques à Isoform Akt :

Cellular Effect

Cell Line	Type	Value	Description	References
HeLa	IC₅₀	1.14 μM Compound: Tilorone	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	[PMID: 32832035]
Oocyte	EC₅₀	2.5 μM Compound: 1	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	[PMID: 22281189]
Vero	CC₅₀	19.67 μM Compound: Tilorone	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	10.1101/2020.03.20.999730
Vero	IC₅₀	4.09 μM Compound: Tilorone	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	10.1101/2020.03.20.999730

In Vitro

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.

Western Blot Analysis^[3]

Cell Line:

Myoblasts
Concentration:

20 nM, 35 nM
Incubation Time:

40 h
Result:

Increased the phosphorylation of Smad1/5/8, indicating the enhancement of BMP signaling.

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].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

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 100 μL saline via the lateral tail vein
Result:

Significant increased in the SUV mean of skeletal muscle, adipose tissue, and liver.

Chemical Information

CAS No. 27591-97-5
Appearance Solid
Masse moléculaire 410.55
Formule C₂₅H₃₄N₂O₃
Color Orange to red
SMILES

O=C1C2=C(C3=C1C=C(OCCN(CC)CC)C=C3)C=CC(OCCN(CC)CC)=C2
Livraison

Room temperature in continental US; may vary elsewhere.
Stockage

-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

Biomed J

Repurposing old drugs as antiviral agents for coronaviruses. [Abstract]

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

Solvant et solubilité

In Vitro:

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)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

2.4358 mL

12.1788 mL

24.3576 mL

5 mM

0.4872 mL

2.4358 mL

4.8715 mL

10 mM

0.2436 mL

1.2179 mL

2.4358 mL

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.

Calculateur de molarité

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

Concentration Concentration

Volume Volume

Molecular Weight Molecular Weight

Calculateur de dilution

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

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In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

Stock Solution Working Solution

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.

Protocol 1

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.

Protocol 2

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.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

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mg/kg
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g
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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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

Pureté et documentation

Select Batch:

Pureté: 99.98%

Assay: 99.98%

ee.: 99.98%

Fiche technique (276 KB)
SDS (252 KB)
- English - EN (252 KB)
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- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
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COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Instruction de manipulation (2659 KB)

Références

[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]

[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.

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

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

Keywords

Tilorone

2 Cited Publications

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Tilorone

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Publications Citing Use of MedChemExpress (MCE) Tilorone

Voir tous les produits spécifiques à Isoform Akt

Activité biologique

Chemical Information

Publications (2)

Solvant et solubilité

Pureté et documentation

Références

Help & FAQs

Complete Stock Solution Preparation Table

Tilorone Related Classifications

HY-B1080A Related Classifications