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Clevudine

🥰Excellent
Catalog No. T6446Cas No. 163252-36-6
Alias 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.

Clevudine

Clevudine

🥰Excellent
Purity: 99.97%
Catalog No. T6446Alias L-FMAU, LevovirCas No. 163252-36-6
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.
Pack SizePriceAvailabilityQuantity
5 mg$47In Stock
10 mg$72In Stock
25 mg$128In Stock
50 mg$207In Stock
100 mg$369In Stock
1 mL x 10 mM (in DMSO)$80In Stock
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Purity:99.97%
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Product Introduction

Bioactivity
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]
AliasL-FMAU, Levovir
Chemical Properties
Molecular Weight260.22
FormulaC10H13FN2O5
Cas No.163252-36-6
SmilesCc1cn([C@H]2O[C@@H](CO)[C@H](O)[C@H]2F)c(=O)[nH]c1=O
Relative Density.1.55g/cm3
Storage & Solubility Information
StoragePowder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice.
Solubility Information
H2O: 48 mg/mL (184.5 mM)
DMSO: 49 mg/mL (188.3 mM)
Ethanol: 4 mg/mL (15.37 mM)
Solution Preparation Table
Ethanol/H2O/DMSO
1mg5mg10mg50mg
1 mM3.8429 mL19.2145 mL38.4290 mL192.1451 mL
5 mM0.7686 mL3.8429 mL7.6858 mL38.4290 mL
10 mM0.3843 mL1.9215 mL3.8429 mL19.2145 mL
H2O/DMSO
1mg5mg10mg50mg
20 mM0.1921 mL0.9607 mL1.9215 mL9.6073 mL
50 mM0.0769 mL0.3843 mL0.7686 mL3.8429 mL
100 mM0.0384 mL0.1921 mL0.3843 mL1.9215 mL

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