同义名 :	L-FMAU; Levovir
	CAS号 :	163252-36-6
	货号 :	A113960
	分子式 :	C10H13FN2O5
	纯度 :	99%+
	分子量 :	260.22
	MDL号 :	MFCD00935785
	存储条件：	Pure form Inert atmosphere, 2-8°C In solvent -20°C:3-6个月-80°C:12个月
	溶解度 :	-
	动物实验配方：

生物活性

描述

Clevudine, a nucleoside analog of the unnatural L-configuration, has potent anti-HBV activity with long half-life, low toxicity. Clevudine is a non-competitive inhibitor that is not incorporated into the viral DNA but rather binds to the polymerase[3]. Clevudine (CLV) has potent anti-hepatitis B virus (HBV) activity in vitro and in vivo with a favorable toxicity profile in all species tested. In cell culture, CLV is readily phosphorylated to the corresponding 5'-triphosphate form of the compound[4]. Clevudine showed a potent antiviral response, and its effect was higher in HBeAg-negative patients, with rapid viral load reduction after therapy[5]. A 24-week clevudine therapy was well-tolerated and showed potent and sustained antiviral effect without evidence of viral resistance in e-CHB (chronic hepatitis B) patients[6].

实验方案
	1mg	5mg	10mg
1 mM 5 mM 10 mM	3.84mL 0.77mL 0.38mL	19.21mL 3.84mL 1.92mL	38.43mL 7.69mL 3.84mL

参考文献

[1]Hu R, Li L, 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 May;49(5):2044-9. [2]Chong Y, Chu CK. Understanding the unique mechanism of L-FMAU (clevudine) against hepatitis B virus: molecular dynamics studies. Bioorg Med Chem Lett. 2002 Dec 2;12(23):3459-62. [3]Asselah T, Lada O, Moucari R, Marcellin P. Clevudine: a promising therapy for the treatment of chronic hepatitis B. Expert Opin Investig Drugs. 2008 Dec;17(12):1963-74 [4]Korba BE, Furman PA, Otto MJ. Clevudine: a potent inhibitor of hepatitis B virus in vitro and in vivo. Expert Rev Anti Infect Ther. 2006 Aug;4(4):549-61 [5]Jang JH, Kim JW, Jeong SH, Myung HJ, Kim HS, Park YS, Lee SH, Hwang JH, Kim N, Lee DH. Clevudine for chronic hepatitis B: antiviral response, predictors of response, and development of myopathy. J Viral Hepat. 2011 Feb;18(2):84-90 [6]Yoo BC, Kim JH, Kim TH, Koh KC, Um SH, Kim YS, Lee KS, Han BH, Chon CY, Han JY, Ryu SH, Kim HC, Byun KS, Hwang SG, Kim BI, Cho M, Yoo K, Lee HJ, Hwang JS, Kim YS, Lee YS, Choi SK, Lee YJ, Yang JM, Park JW, Lee MS, Kim DG, Chung YH, Cho SH, Choi JY, Kweon YO, Lee HY, Jeong SH, Yoo HW, Lee HS. Clevudine is highly efficacious in hepatitis B e antigen-negative chronic hepatitis B with durable off-therapy viral suppression. Hepatology. 2007 Oct;46(4):1041-8