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Tilorone dihydrochloride

MCE China：Tilorone dihydrochloride

Brand：MedChemExpress (MCE)

Cat. No.HY-B1080

CAS：27591-69-1

Purity：99.29%

Storage：4°C, sealed storage, away from moisture *In solvent : -80°C, 1 year; -20°C, 6 months (sealed storage, away from moisture)

Shipping：Room temperature in continental US; may vary elsewhere.

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.Tilorone dihydrochloride exhibits an inhibitory activity with EC50 of 230 nM against Ebola virus (EBOV).

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].

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 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

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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]