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Clevudine

Catalog No. T6446 CAS 163252-36-6

Synonyms: L-FMAU, Levovir

Clevudine (Levovir) is a synthetic pyrimidine analogue with activity against hepatitis B virus (HBV). Intracellularly, clevudine is phosphorylated to its active metabolites, clevudine monophosphate and triphosphate. The triphosphate metabolite competes with thymidine for incorporation into viral DNA, thereby causing DNA chain termination and inhibiting the function of HBV DNA polymerase (reverse transcriptase). Clevudine has a long half-life and shows significant reduction of covalently closed circular DNA (cccDNA), therefore the patient is less likely to have a relapse after treatment is discontinued.

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Clevudine, CAS 163252-36-6

Pack Size	Availability	Price/USD
5 mg	In stock	$ 47.00
10 mg	In stock	$ 72.00
25 mg	In stock	$ 128.00
50 mg	In stock	$ 207.00
100 mg	In stock	$ 369.00
1 mL * 10 mM (in DMSO)	In stock	$ 80.00

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Purity: 99.98%

Purity: 99.88%

Biological Description

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Storage & Solubility Information

Description	Clevudine (Levovir) is a synthetic pyrimidine analogue with activity against hepatitis B virus (HBV). Intracellularly, clevudine is phosphorylated to its active metabolites, clevudine monophosphate and triphosphate. The triphosphate metabolite competes with thymidine for incorporation into viral DNA, thereby causing DNA chain termination and inhibiting the function of HBV DNA polymerase (reverse transcriptase). Clevudine has a long half-life and shows significant reduction of covalently closed circular DNA (cccDNA), therefore the patient is less likely to have a relapse after treatment is discontinued.
In vitro	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. [1] 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. [2] Clevudine is readily phosphorylated to the corresponding 5'-triphosphate form of the compound in cell culture, which involves the mechanism of action of Clevudine. [3]
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. [1] 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. [2] Clevudine is readily phosphorylated to the corresponding 5'-triphosphate form of the compound in cell culture, which involves the mechanism of action of Clevudine. [3]

Synonyms	L-FMAU, Levovir
Molecular Weight	260.22
Formula	C10H13FN2O5
CAS No.	163252-36-6

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

H2O: 48 mg/mL (184.5 mM)

DMSO: 49 mg/mL (188.3 mM)

Ethanol: 4 mg/mL (15.37 mM)

References and Literature

1. Chong Y, et al. Bioorg Med Chem Lett, 2002, 12(23), 3459-3462. 2. Hu R, et al. Antimicrob Agents Chemother, 2005, 49(5), 2044-2049. 3. Korba BE, et al. Expert Rev Anti Infect Ther, 2006, 4(4), 549-561. 4. Jacquard AC, et al. Antimicrob Agents Chemother, 2004, 48(7), 2683-2692.

Related compound libraries

This product is contained In the following compound libraries：

Drug Repurposing Compound Library Anti-Cancer Clinical Compound Library Anti-Cancer Approved Drug Library Anti-Cancer Drug Library Inhibitor Library Anti-Cancer Compound Library Approved Drug Library NO PAINS Compound Library Anti-Viral Compound Library Covalent Inhibitor Library

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Keywords

Clevudine 163252-36-6 Cell Cycle/Checkpoint DNA Damage/DNA Repair Microbiology/Virology HBV DNA/RNA Synthesis Orthopoxvirus half-life L-FMAU nucleoside analog Inhibitor polymerase Hepatitis B virus low toxicity inhibit Levovir inhibitor

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