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Chemical Structure| 27591-69-1 Chemical Structure| 27591-69-1

Structure of Tilorone 2HCl
CAS No.: 27591-69-1

Chemical Structure| 27591-69-1

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Tilorone 2HCl is an orally active interferon inducer, used as an antiviral drug.

Synonyms: Tilorone (hydrochloride); Tilorone dihydrochloride; NSC 143969

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Product Details of Tilorone 2HCl

CAS No. :27591-69-1
Formula : C25H36Cl2N2O3
M.W : 483.47
SMILES Code : O=C1C2=C(C3=C1C=C(OCCN(CC)CC)C=C3)C=CC(OCCN(CC)CC)=C2.[H]Cl.[H]Cl
Synonyms :
Tilorone (hydrochloride); Tilorone dihydrochloride; NSC 143969
MDL No. :MFCD00134071
InChI Key :BSVYJQAWONIOOU-UHFFFAOYSA-N
Pubchem ID :33958

Safety of Tilorone 2HCl

GHS Pictogram:
Signal Word:Warning
Hazard Statements:H302+H312+H332-H315-H319-H335-H351
Precautionary Statements:P201-P202-P261-P264-P270-P271-P280-P301+P312+P330-P302+P352+P312-P304+P340+P312-P305+P351+P338-P308+P313-P332+P313-P337+P313-P403+P233-P405-P501

Isoform Comparison

Biological Activity

In Vitro:

Cell Line
Concentration Treated Time Description References
A549 cells 6.31 µM 24 hours Evaluate the inhibitory effect of Tilorone on RVFV ZH501, showing an EC50 of 6.31 μM Microorganisms. 2021 Dec 31;10(1):92
Vero CCL81 cells 6.45 µM 24 hours Evaluate the inhibitory effect of Tilorone on RVFV ZH501, showing an EC50 of 6.45 μM Microorganisms. 2021 Dec 31;10(1):92
A549 cells 1.41 µM 24 hours Evaluate the inhibitory effect of Tilorone on RVFV MP-12, showing an EC50 of 1.41 μM Microorganisms. 2021 Dec 31;10(1):92
Vero CCL81 cells 0.67 µM 24 hours Evaluate the inhibitory effect of Tilorone on RVFV MP-12, showing an EC50 of 0.67 μM Microorganisms. 2021 Dec 31;10(1):92
Human midbrain-like organoids 0.5 µM to 4 µM 48 hours Assess the effect of Tilorone on the uptake of α-syn fibrils and apoptosis. Results showed that Tilorone reduced the uptake of α-syn fibrils and mitigated α-syn fibril-induced apoptosis. Furthermore, Tilorone reduced sPFF-induced endogenous α-syn phosphorylation. J Transl Med. 2024 Sep 2;22(1):816
Bovine corneal fibroblasts 5 µM 96 hours Investigation of tilorone-induced lysosomal storage of glycosaminoglycans (GAGs), showing predominant accumulation of dermatan sulfate (DS), accounting for over 90% of intracellular GAG storage. Biochem J. 1995 Nov 15;312 ( Pt 1)(Pt 1):215-22
Mouse primary hippocampal neurons 0.5 µM to 2 µM two weeks Evaluate the effect of Tilorone on the uptake of α-syn fibrils and endogenous α-syn phosphorylation. Results showed that Tilorone reduced the uptake of α-syn fibrils in a dose-dependent manner, with maximal inhibition observed at 2 µM. Additionally, Tilorone reduced sPFF-induced endogenous α-syn phosphorylation. J Transl Med. 2024 Sep 2;22(1):816

In Vivo:

Species
Animal Model
Administration Dosage Frequency Description References
ICR mice Lethal virus challenge model Intraperitoneal injection 20 mg/kg Once daily for 7 days To evaluate the in vivo antiviral efficacy of tilorone against SFTSV, results showed that 20 mg/kg tilorone protected 78.94% of mice from lethal challenge Virol Sin. 2022 Feb;37(1):145-148
CD-1 mice VEEV infection model Intragastric 25.6 mg/kg Once daily for 10 days Tilorone significantly reduced viremia in mice and protected them from death Pharmaceuticals (Basel). 2022 May 17;15(5):617
Mice SPF mice Oral 250 mg/kg Single dose, observed for 24 hours To evaluate the IFN-α inducing activity of tilorone dihydrochloride, showing peak levels (approximately 2000 pg/mL) at 12 to 24 hours post-administration. Molecules. 2015 Dec 2;20(12):21458-63
BALB/c mice RVFV ZH501 infection model Intraperitoneal injection 30 mg/kg/day or 60 mg/kg/day Once daily for 9 days Evaluate the in vivo protective effect of Tilorone against RVFV ZH501 infection, showing 80% survival at 30 mg/kg/day Microorganisms. 2021 Dec 31;10(1):92
Mice CD-1 mice Oral 75 mg/kg Single dose To study the effect of Tilorone on the expression of xanthine dehydrogenase (XD) mRNA in mouse liver. Results showed that Tilorone increased the expression of XD mRNA. Biochem J. 1992 May 1;283 ( Pt 3)(Pt 3):863-70

Protocol

Bio Calculators
Preparing Stock Solutions 1mg 5mg 10mg

1 mM

5 mM

10 mM

2.07mL

0.41mL

0.21mL

10.34mL

2.07mL

1.03mL

20.68mL

4.14mL

2.07mL

References

 

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