Powder: -20°C for 3 years | In solvent: -80°C for 1 year
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。
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 |
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 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
H2O: 48 mg/mL (184.5 mM)
DMSO: 49 mg/mL (188.3 mM)
Ethanol: 4 mg/mL (15.37 mM)
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 |
对于不同动物的给药剂量换算,您也可以参考 更多...
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。
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。
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 克拉夫定 toxicity inhibit Levovir inhibitor