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Clevudine

Clevudine

产品编号 T6446   CAS 163252-36-6
别名: L-FMAU, 克拉夫定, Levovir

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。

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Clevudine Chemical Structure
Clevudine, CAS 163252-36-6
规格 价格/CNY 货期 数量
5 mg ¥ 169 现货
10 mg ¥ 233 现货
25 mg ¥ 372 现货
50 mg ¥ 538 现货
100 mg ¥ 788 现货
1 mL * 10 mM (in DMSO) ¥ 597 现货
其他形式的 Clevudine:
产品目录号及名称: Clevudine (T6446)
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生物活性
化学信息
存储 & 溶解度
参考文献
产品描述 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.
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]
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]
别名 L-FMAU, 克拉夫定, Levovir
分子量 260.22
分子式 C10H13FN2O5
CAS No. 163252-36-6

存储

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

溶解度

H2O: 48 mg/mL (184.5 mM)

DMSO: 49 mg/mL (188.3 mM)

Ethanol: 4 mg/mL (15.37 mM)

溶液配制表

可选溶剂 浓度 体积 质量 1 mg 5 mg 10 mg 25 mg
H2O / DMSO / Ethanol 1 mM 3.8429 mL 19.2145 mL 38.429 mL 96.0726 mL
5 mM 0.7686 mL 3.8429 mL 7.6858 mL 19.2145 mL
10 mM 0.3843 mL 1.9215 mL 3.8429 mL 9.6073 mL
H2O / DMSO 20 mM 0.1921 mL 0.9607 mL 1.9215 mL 4.8036 mL
50 mM 0.0769 mL 0.3843 mL 0.7686 mL 1.9215 mL
100 mM 0.0384 mL 0.1921 mL 0.3843 mL 0.9607 mL

计算器

摩尔浓度计算器
稀释计算器
配液计算器
分子量计算器
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输入分子式,点击计算,可计算出产品的分子量。

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.
Urolithin A Cytarabine hydrochloride Amuvatinib Triazavirin RG7800 Hydroxyurea L67 Dehydroaltenusin

相关化合物库

该产品包含在如下化合物库中:
抗癌上市药物库 抗癌药物库 抗癌临床化合物库 已知活性化合物库 抗衰老化合物库 抗癌化合物库 上市药物库 抗COVID-19化合物库 DNA 损伤和修复分子库 药物功能重定位化合物库

剂量换算

对于不同动物的给药剂量换算,您也可以参考 更多...

体内实验配液计算器

请在以下方框中输入您的动物实验信息后点击计算,可以得到母液配置方法和体内配方的制备方法: 比如您的给药剂量是10 mg/kg,每只动物体重20 g,给药体积100 μL,一共给药动物10 只,您使用的配方为5% DMSO+30% PEG300+5% Tween 80+60% ddH2O。那么您的工作液浓度为2 mg/mL。

母液配置方法:2 mg 药物溶于 50 μL DMSO (母液浓度为 40 mg/mL), 如您需要配置的浓度超过该产品的溶解度,请先与我们联系。

体内配方的制备方法:取 50 μL DMSO 主液,加入 300 μL PEG300, 混匀澄清,再加 50 μL Tween 80,混匀澄清,再加 600 μL ddH2O, 混匀澄清。

第一步:请输入动物实验的基本信息
剂量
mg/kg
每只动物体重
g
给药体积
μL
动物数量
第二步:请输入动物体内配方组成,不同的产品配方组成不同,如有配方需求,可先联系我们提供正确的体内配方。
% DMSO
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% Tween 80
% ddH2O
计算 重置

技术支持

您可能有的问题的答案可以在抑制剂处理说明中找到,包括如何准备库存溶液,如何存储产品,以及基于细胞的分析和动物实验需要特别注意的问题。

Keywords

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

 

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