Tilorone dihydrochloride is a first-in-class, orally bioavailable interferon inducer, with antiviral, antineoplastic, and anti-inflammatory activity, it can inhibit Ebola virus (EBOV).

Physicochemical Properties

Molecular Formula	C25H36CL2N2O3
Molecular Weight	483.474
Exact Mass	482.21
CAS #	27591-69-1
Related CAS #	27591-69-1;
PubChem CID	33958
Appearance	Light yellow to orange solid powder
Density	1.102g/cm3
Boiling Point	552.3ºC at 760 mmHg
Melting Point	230-233 °C(lit.)
Flash Point	287.8ºC
Vapour Pressure	3.05E-12mmHg at 25°C
LogP	5.943
Hydrogen Bond Donor Count	2
Hydrogen Bond Acceptor Count	5
Rotatable Bond Count	12
Heavy Atom Count	32
Complexity	477
Defined Atom Stereocenter Count	0
SMILES	Cl[H].Cl[H].O(C([H])([H])C([H])([H])N(C([H])([H])C([H])([H])[H])C([H])([H])C([H])([H])[H])C1C([H])=C([H])C2=C(C=1[H])C(C1C([H])=C(C([H])=C([H])C2=1)OC([H])([H])C([H])([H])N(C([H])([H])C([H])([H])[H])C([H])([H])C([H])([H])[H])=O
InChi Key	BSVYJQAWONIOOU-UHFFFAOYSA-N
InChi Code	InChI=1S/C25H34N2O3.2ClH/c1-5-26(6-2)13-15-29-19-9-11-21-22-12-10-20(30-16-14-27(7-3)8-4)18-24(22)25(28)23(21)17-19/h9-12,17-18H,5-8,13-16H2,1-4H32*1H
Chemical Name	2,7-Bis[2-(diethylamino)ethoxy]fluoren-9-one dihydrochloride
Synonyms	Tilorone dihydrochloride
HS Tariff Code	2934.99.9001
Storage	Powder-20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month Note: Please store this product in a sealed and protected environment, avoid exposure to moisture.
Shipping Condition	Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)

Biological Activity

References

Ekins S, Lingerfelt MA, Comer JE, Freiberg AN, Mirsalis JC, O'Loughlin K, Harutyunyan A, McFarlane C, Green CE, Madrid PB. Efficacy of Tilorone Dihydrochloride against Ebola Virus Infection. Antimicrob Agents Chemother. 2017 Nov 13. pii: AAC.01711-17. doi: 10.1128/AAC.01711-17. [Epub ahead of print] PubMed PMID: 29133569.

Additional Infomation

Tilorone dihydrochloride is the dihydrochloride salt of tilorone. It is used as an antiviral drug to treat influenza, herpes infection, viral hepatitis, acute respiratory viral infections and SARS. It has a role as an anti-inflammatory agent, an antineoplastic agent, an interferon inducer, a nicotinic acetylcholine receptor agonist and an antiviral drug. It contains a tilorone(2+). An antiviral agent used as its hydrochloride. It is the first recognized synthetic, low-molecular-weight compound that is an orally active interferon inducer, and is also reported to have antineoplastic and anti-inflammatory actions.

Solubility Data

Solubility (In Vitro)

H2O : ~100 mg/mL (~206.84 mM) DMSO : ~12.5 mg/mL (~25.85 mM)

Solubility (In Vivo)

Solubility in Formulation 1: ≥ 1.25 mg/mL (2.59 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 12.5 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 1.25 mg/mL (2.59 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 12.5 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. Solubility in Formulation 3: 25 mg/mL (51.71 mM) in PBS (add these co-solvents sequentially from left to right, and one by one), clear solution; with ultrasonication.  (Please use freshly prepared in vivo formulations for optimal results.)

Preparing Stock Solutions		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

*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.