Cridanimod
(Synonyms: 吖啶酮乙酸) 目录号 : GC38648An inducer of type I interferon production
Cas No.:38609-97-1
Sample solution is provided at 25 µL, 10mM.
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Cridanimod is an inducer of type I interferon (IFN) production.1,2 It induces IRF3 phosphorylation, IFN-β production, and NF-κB activation in wild-type, but not in stimulator of interferon genes (STING) mutant, murine macrophages.1 In vivo, cridanimod (112-1,792 mg/kg) increases plasma levels of IFN in weanling and adult mice.2 Cridanimod inhibits viral infection in mouse models of Semliki forest, coxsackie B1, Columbia SK, herpes, and pseudorabies viruses with protective doses (PD50s) ranging from 17-320 mg/kg.3 It increases uterine expression of estrogen and progesterone receptors in ovariectomized rats.4 Cridanimod also reverses tamoxifen-induced decreases in progesterone receptor expression in young rats.
1.Cavlar, T., Deimling, T., Ablasser, A., et al.Species-specific detection of the antiviral small-molecule compound CMA by STINGEMBO J.32(10)1440-1450(2013) 2.Taylor, J.L., Schoenherr, C.K., and Grossberg, S.E.High-yield interferon induction by 10-carboxymethyl-9-acridanone in mice and hamstersAntimicrob. Agents Chemother.18(1)20-26(1980) 3.Kramer, M.J., Cleeland, R., and Grunberg, E.Antiviral activity of 10-carboxymethyl-9-acridanoneAntimicrob. Agents Chemother.9(2)233-238(1976) 4.Surkov, K.G., Tsyrlina, E.V., Konstantinova, M.M., et al.Neovir, an interferon inductor, modifies expression of steroid hormone receptors in hormone-dependent tissues and restores sensitivity to tamoxifen in patients with inoperable breast cancerVopr. Onkol.42(6)28-32(1996)
Cas No. | 38609-97-1 | SDF | |
别名 | 吖啶酮乙酸 | ||
Canonical SMILES | O=C(O)CN(C1=C2C=CC=C1)C3=CC=CC=C3C2=O | ||
分子式 | C15H11NO3 | 分子量 | 253.26 |
溶解度 | DMSO: 125 mg/mL (493.56 mM); Water: < 0.1 mg/mL (insoluble) | 储存条件 | Store at -20°C |
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1 mg | 5 mg | 10 mg | |
1 mM | 3.9485 mL | 19.7426 mL | 39.4851 mL |
5 mM | 0.7897 mL | 3.9485 mL | 7.897 mL |
10 mM | 0.3949 mL | 1.9743 mL | 3.9485 mL |
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Tilorone and Cridanimod Protect Mice and Show Antiviral Activity in Rats despite Absence of the Interferon-Inducing Effect in Rats
Pharmaceuticals (Basel) 2022 May 17;15(5):617.PMID:35631443DOI:10.3390/ph15050617.
The synthetic compounds, Tilorone and Cridanimod, have the antiviral activity which initially had been ascribed to the capacity to induce interferon. Both drugs induce interferon in mice but not in humans. This study investigates whether these compounds have the antiviral activity in mice and rats since rats more closely resemble the human response. Viral-infection models were created in CD-1 mice and Wistar rats. Three strains of Venezuelan equine encephalitis virus were tested for the performance in these models. One virus strain is the molecularly cloned attenuated vaccine. The second strain has major virulence determinants converted to the wild-type state which are present in virulent strains. The third virus has wild-type virulence determinants, and in addition, is engineered to express green fluorescent protein. Experimentally infected animals received Tilorone or Cridanimod, and their treatment was equivalent to the pharmacopoeia-recomended human treatment regimen. Tilorone and Cridanimod show the antiviral activity in mice and rats and protect the mice from death. In rats, both drugs diminish the viremia. These drugs do not induce interferon-alpha or interferon-beta in rats. The presented observations allow postulating the existence of an interferon-independent and species-independent mechanism of action.