Fialuridine (CAS 69123-98-4)
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Fialuridine (FIAU), also known as DRG-0098, is a nucleoside analog that exhibits antiviral properties. It effectively inhibits thymidine kinases from herpes simplex virus types 1 and 2, with Ki values of 0.14 µM and 0.95 µM, respectively. However, its inhibitory effect on green monkey Vero cell thymidine kinase is less pronounced, with a Ki value of 53 µM. Fialuridine hinders DNA synthesis in human cytomegalovirus, hepatitis B, and herpes simplex. It is important to note that while Fialuridine demonstrates minimal adverse effects in various mammals, it can lead to liver damage and fatality in humans due to its mitochondrial toxicity. Fialuridine is phosphorylated and inhibits DNA synthesis in isolated rat hepatic mitochondria. Moreover, Fialuridine and its metabolites impede DNA polymerase gamma at sites where multiple adjacent analogs are incorporated, resulting in reduced mtDNA abundance and causing structural defects in cultured hepatoblasts.
Fialuridine (CAS 69123-98-4) References
- Identification of the mitochondrial targeting signal of the human equilibrative nucleoside transporter 1 (hENT1): implications for interspecies differences in mitochondrial toxicity of fialuridine. | Lee, EW., et al. 2006. J Biol Chem. 281: 16700-6. PMID: 16595656
- Incorporation of fialuridine (FIAU) into mitochondrial DNA and effects of FIAU on the morphology of mitochondria in human hepatoblastoma cells. | Colacino, JM., et al. 1996. Toxicol In Vitro. 10: 297-303. PMID: 20650209
- Fialuridine induces acute liver failure in chimeric TK-NOG mice: a model for detecting hepatic drug toxicity prior to human testing. | Xu, D., et al. 2014. PLoS Med. 11: e1001628. PMID: 24736310
- Mechanisms of Chronic Fialuridine Hepatotoxicity as Revealed in Primary Human Hepatocyte Spheroids. | Hendriks, DFG., et al. 2019. Toxicol Sci. 171: 385-395. PMID: 31505000
- Priming of duck hepatitis B virus reverse transcription in vitro: premature termination of primer DNA induced by the 5'-triphosphate of fialuridine. | Staschke, KA. and Colacino, JM. 1994. J Virol. 68: 8265-9. PMID: 7525986
- Hepatic failure and lactic acidosis due to fialuridine (FIAU), an investigational nucleoside analogue for chronic hepatitis B. | McKenzie, R., et al. 1995. N Engl J Med. 333: 1099-105. PMID: 7565947
- Effect of fialuridine on replication of mitochondrial DNA in CEM cells and in human hepatoblastoma cells in culture. | Colacino, JM., et al. 1994. Antimicrob Agents Chemother. 38: 1997-2002. PMID: 7811009
- Sensitive and specific radioimmunoassay for fialuridine: initial assessment of pharmacokinetics after single oral doses to healthy volunteers. | Bowsher, RR., et al. 1994. Antimicrob Agents Chemother. 38: 2134-42. PMID: 7811032
- Fialuridine accumulates in DNA of dogs, monkeys, and rats following long-term oral administration. | Richardson, FC., et al. 1994. Proc Natl Acad Sci U S A. 91: 12003-7. PMID: 7991573
- Mechanisms for the anti-hepatitis B virus activity and mitochondrial toxicity of fialuridine (FIAU). | Colacino, JM. 1996. Antiviral Res. 29: 125-39. PMID: 8739593
- Comparison of the DNA incorporation in human MOLT-4 cells of two 2'-beta-fluoronucleosides, 2'-beta-fluoro-2',3'-dideoxyadenosine and fialuridine. | Ahluwalia, GS., et al. 1996. J Pharm Sci. 85: 454-5. PMID: 8901088
- Histopathologic changes associated with fialuridine hepatotoxicity. | Kleiner, DE., et al. 1997. Mod Pathol. 10: 192-9. PMID: 9071726
- Fialuridine is phosphorylated and inhibits DNA synthesis in isolated rat hepatic mitochondria. | Horn, DM., et al. 1997. Antiviral Res. 34: 71-4. PMID: 9107387
- Mitochondrial injury. Lessons from the fialuridine trial. | Honkoop, P., et al. 1997. Drug Saf. 17: 1-7. PMID: 9258627
Ordering Information
| Product Name | Catalog # | UNIT | Price | Qty | FAVORITES | |
Fialuridine, 10 mg | sc-221614 | 10 mg | $300.00 | |||
Fialuridine, 100 mg | sc-221614A | 100 mg | $1950.00 | |||
Fialuridine, 1 g | sc-221614B | 1 g | $4000.00 | |||
Fialuridine, 10 g | sc-221614C | 10 g | $24000.00 | |||
Fialuridine, 50 g | sc-221614D | 50 g | $31500.00 | |||
Fialuridine, 100 g | sc-221614E | 100 g | $39500.00 |