product name Clevudine
Description: Clevudine is a potent antiviral drug for the treatment of hepatitis B with EC50 0.1 μM in HepG2 2.2.15 cells as well as EBV, it has low cytotoxicities in a variety of cell lines including MT2, CEM, H1 and HepG2 2.2.15 and bone marrow progenitor cells. Clevudine is metabolized in cells by the cellular thymidine kinase as well as deoxycytidine kinase to its monophosphate, and subsequently to the di- and triphosphate.
References: Bioorg Med Chem Lett. 2002 Dec 2;12(23):3459-62; Antimicrob Agents Chemother. 2005 May;49(5):2044-9.
260.22
Formula
C10H13FN2O5
CAS No.
163252-36-6
Storage
-20℃ for 3 years in powder form
-80℃ for 2 years in solvent
Solubility (In vitro)
DMSO: 52 mg/mL (199.8 mM)
Water: 52 mg/mL (199.8 mM) <1 mg/mL
Ethanol: 4 mg/mL (15.4 mM)
Solubility (In vivo)
Synonyms
other peoduct :References PubMed ID：:http://www.ncbi.nlm.nih.gov/pubmed/19413393
| In Vitro |
In vitro activity: Clevudine is a potent antiviral agent against HBV (EC50 0.1 μM in HepG2 2.2.15 cells) as well as EBV, which has low cytotoxicities in a variety of cell lines including MT2, CEM, H1 and HepG2 2.2.15 and bone marrow progenitor cells. Clevudine is metabolized in cells by the cellular thymidine kinase as well as deoxycytidine kinase to its monophosphate, and subsequently to the di- and triphosphate. Clevudine is known to act specifically on viral DNA synthesis, and its triphosphate inhibits the HBV DNA synthesis in a dose-dependent manner without being incorporated into the DNA or chain termination. Clevudine results in increase of the amounts of the diphosphate and triphosphate metabolites of these analogs. Clevudine monophosphate (L-FMAUMP) is a poorer substrate than its D-configuration anomer. Clevudine is readily phosphorylated to the corresponding 5-triphosphate form of the compound in cell culture, which involves the mechanism of action of Clevudine. Kinase Assay: Cell Assay: |
|---|---|
| In Vivo | Clevudine is a potent antiviral agent against HBV (EC50 0.1 μM in HepG2 2.2.15 cells) as well as EBV, which has low cytotoxicities in a variety of cell lines including MT2, CEM, H1 and HepG2 2.2.15 and bone marrow progenitor cells. Clevudine is metabolized in cells by the cellular thymidine kinase as well as deoxycytidine kinase to its monophosphate, and subsequently to the di- and triphosphate. Clevudine is known to act specifically on viral DNA synthesis, and its triphosphate inhibits the HBV DNA synthesis in a dose-dependent manner without being incorporated into the DNA or chain termination. Clevudine results in increase of the amounts of the diphosphate and triphosphate metabolites of these analogs. Clevudine monophosphate (L-FMAUMP) is a poorer substrate than its D-configuration anomer. Clevudine is readily phosphorylated to the corresponding 5-triphosphate form of the compound in cell culture, which involves the mechanism of action of Clevudine. |
| Animal model | |
| Formulation & Dosage | |
| References | Bioorg Med Chem Lett. 2002 Dec 2;12(23):3459-62; Antimicrob Agents Chemother. 2005 May;49(5):2044-9. |
