Tilorone dihydrochloride

Name: Tilorone dihydrochloride
Brand: MedChemExpress
SKU: HY-B1080
Rating: 4.5 (1 reviews)

Cat. No.: HY-B1080 Purity: 99.79%: FAQs
Data Sheet SDS COA Handling Instructions

Molarity Calculator

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.

Tilorone dihydrochloride Chemical Structure

CAS No. : 27591-69-1

Size	Price	Stock	Quantity

Free Sample (0.1 - 0.5 mg)		Apply Now
Solid + Solvent
10 mM * 1 mL in DMSO ready for reconstitution	USD 80	In-stock	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	USD 80	In-stock	Estimated Time of Arrival: December 31
Solid
100 mg	USD 72	In-stock	Estimated Time of Arrival: December 31
500 mg	USD 216	In-stock	Estimated Time of Arrival: December 31
1 g		Get quote
5 g		Get quote

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Customer Review

Based on 1 publication(s) in Google Scholar

Other Forms of Tilorone dihydrochloride:

Tilorone In-stock

1 Publications Citing Use of MCE Tilorone dihydrochloride

•Biomed J. 2020 Aug;43(4):368-374. [Abstract]

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HIF-1α HIF

Biological Activity
Purity & Documentation
References
Customer Review

Description

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^[1]^[2]^[3].Tilorone dihydrochloride exhibits an inhibitory activity with EC₅₀ of 230 nM against Ebola virus (EBOV)^[4].

In Vitro

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.

In Vivo

Tilorone (5-20 mg/kg; intraperitoneally; once daily at 1-7 days) dihydrochloride with 20 mg/kg protects 78.94% of the mice from lethal challenge with virus intracranially^[1].
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	T_1/2 (h)	T_max (h)	C_max (ng/ml)	AUC_last (ng·h/ml)	AUC_inf (ng·h/ml)	CL_blood (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.

Molecular Weight

483.47

Formula

C₂₅H₃₆Cl₂N₂O₃

CAS No.

27591-69-1

Appearance

Solid

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)

Solvent & Solubility

In Vitro:

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)

Preparing
Stock Solutions

Concentration Solvent Mass	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

View the 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.

* 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.

Molarity Calculator
Dilution Calculator

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

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

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

In Vivo:

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.

Protocol 1

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.
Protocol 2

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.

Protocol 1

Add each solvent one by one: PBS
Solubility: 25 mg/mL (51.71 mM); Clear solution; Need ultrasonic

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

Dosing volume
(per animal)

μL

Number of animals

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

Calculation results:

Working solution concentration: mg/mL

This product has good water solubility, please refer to the measured solubility data in water/PBS/Saline for details.

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only.If necessary, please contact MedChemExpress (MCE).

Purity & Documentation

Purity: 99.79%

Select Batch:

Data Sheet (278 KB) SDS (0 KB)

COA (245 KB) LCMS (266 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

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.