貨號	規格	價格	上海	北京	武漢	南京
S80435-5mg	98.3%	￥80.00 S80435-5mg ￥80.00 現貨	9 9	-	-	-
S80435-10mg	98.3%	￥110.00 S80435-10mg ￥110.00 現貨	9 9	-	-	-
S80435-50mg	98.3%	￥380.00 S80435-50mg ￥380.00 現貨	7 7	-	-	-
S80435-250mg	98.3%	￥1190.00 S80435-250mg ￥1190.00 現貨	2 2	-	-	-

產品介紹

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.

產品描述：

靶點：

DNA/RNA Synthesis;HBV;HBV;DNA/RNASynthesis

體外研究：

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. 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. Clevudine is readily phosphorylated to the corresponding 5'-triphosphate form of the compound in cell culture, which involves the mechanism of action of Clevudine.

體內研究：

參考文獻：

1. Korba BE, et al. Clevudine: a potent inhibitor of hepatitis B virus in vitro and in vivo. Expert Rev Anti Infect Ther, 2006, 4(4), 549-561. 2. Jacquard AC, et al. Effect of a combination of clevudine and emtricitabine with adenovirus-mediated delivery of gamma interferon in the woodchuck model of hepatitis B virus infection. Antimicrob Agents Chemother, 2004, 48(7), 2683-2692. 3. Hu R, et al. Behavior of thymidylate kinase toward monophosphate metabolites and its role in the metabolism of 1-(2'-deoxy-2'-fluoro-beta-L-arabinofuranosyl)-5-methyluracil (Clevudine) and 2',3'-didehydro-2',3'-dideoxythymidine in cells. Antimicrob Agents Chemother, 2005, 49(5), 2044-2049. 4. Chong Y, et al. Understanding the unique mechanism of L-FMAU (clevudine) against hepatitis B virus: molecular dynamics studies. Bioorg Med Chem Lett, 2002, 12(23), 3459-3462.

溶解性：

Soluble in DMSO、Ethanol、H2O

保存條件：

2-8℃

配置溶液濃度參考：

	1mg	5mg	10mg
1 mM	3.843 ml	19.215 ml	38.429 ml
5 mM	0.769 ml	3.843 ml	7.686 ml
10 mM	0.384 ml	1.921 ml	3.843 ml
50 mM	0.077 ml	0.384 ml	0.769 ml

注意：

部分產品我司僅能提供部分信息，我司不保證所提供信息的權威性，僅供客戶參考交流研究之用。

參考文獻

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Clevudine

1-((2S,3R,4S,5S)-3-fluoro-4-hydroxy-5-(hydroxymethyl)tetrahydrofuran-2-yl)-5-methylpyrimidine-2,4(1H,3H)-dione