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Clevudine

Clevudine (Levovir) 是一种非自然 L-构型的核苷类似物，是一种与聚合酶结合的非竞争性抑制剂，具有较强的抗 HBV 活性，半衰期长，毒性低的特点。

CAS号

163252-36-6

分子式

C10H13FN2O5

主要靶点

DNA/RNA Synthesis|HBV

仅限科研使用

Cat No : CM04358

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Synonyms

Levovir|克拉夫定|L-FMAU

验证数据展示

  • CAS No.: 163252-36-6

    Clevudine
    CAS#: 163252-36-6

产品信息

Clevudine 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.

CAS号 163252-36-6
分子式 C10H13FN2O5
主要靶点 DNA/RNA Synthesis|HBV
主要通路 细胞周期|DNA损伤和修复|微生物学
分子量 260.22
纯度 99.88%， 此纯度可做参考，具体纯度与批次有关系，可咨询客服
储存条件 Powder: -20°C for 3 years | In solvent: -80°C for 1 year
别名 Levovir|克拉夫定|L-FMAU

体内活性

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]

体外活性

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]

溶解度

Ethanol:4 mg/mL (15.37 mM),DMSO:49 mg/mL (188.3 mM),H2O:48 mg/mL (184.5 mM)

参考文献

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.

The molarity calculator equation

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

质量   浓度   体积   分子量 *
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The dilution calculator equation

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
This equation is commonly abbreviated as: C1V1 = C2V2

浓度 (start) × 体积 (start) = 浓度 (final) × 体积 (final)
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C1   V1   C2   V2