| CAS NO: | 163252-36-6 |
| 规格: | ≥98% |
| 包装 | 价格(元) |
| 5mg | 电议 |
| 10mg | 电议 |
| 25mg | 电议 |
| 50mg | 电议 |
| 100mg | 电议 |
| 250mg | 电议 |
| 500mg | 电议 |
| Molecular Weight (MW) | 260.22 |
|---|---|
| Formula | C10H13FN2O5 |
| CAS No. | 163252-36-6 (Clevudine); |
| 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) | |
| Other info | Chemical Name:
1-((2S,3R,4S,5S)-3-fluoro-4-hydroxy-5-(hydroxymethyl)tetrahydrofuran-2-yl)-5-methylpyrimidine-2,4(1H,3H)-dione InChi Key: GBBJCSTXCAQSSJ-XQXXSGGOSA-N InChi Code: InChI=1S/C10H13FN2O5/c1-4-2-13(10(17)12-8(4)16)9-6(11)7(15)5(3-14)18-9/h2,5-7,9,14-15H,3H2,1H3,(H,12,16,17)/t5-,6+,7-,9-/m0/s1 SMILES Code: O=C1NC(C(C)=CN1[C@@H]2[C@H](F)[C@H]([C@H](CO)O2)O)=O |
| Synonyms | L-FMAU; L FMAU; LFMAU |
| 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. |
|---|---|
| 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 | N/A |
| Formulation & Dosage | N/A |
| References | Bioorg Med Chem Lett. 2002 Dec 2;12(23):3459-62; Antimicrob Agents Chemother. 2005 May;49(5):2044-9. |
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