产品说明书

Entecavir Monohydrate

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Chemical Structure| 209216-23-9 同义名 : 恩替卡韦一水合物 ;BMS200475 monohydrate;SQ34676 monohydrate;SQ 34,676;BMS 200475;Entecavir (hydrate);Entecavir Hydrate
CAS号 : 209216-23-9
货号 : A148639
分子式 : C12H17N5O4
纯度 : 98%
分子量 : 295.295
MDL号 : MFCD09754448
存储条件:

粉末 Keep in dark place,Inert atmosphere,Room temperature

液体 -20°C:3-6个月-80°C:12个月

溶解度 :

DMSO: 50 mg/mL(169.32 mM),注意:DMSO长时间开封后,会吸水并导致溶解能力下降,请避免使用长期开封的DMSO

H2O: 2.5 mg/mL(8.47 mM)

动物实验配方:
生物活性
描述 Entecavir (ETV) Monohydrate is a first-line therapy for chronic hepatitis B virus (HBV), demonstrating potent suppression of HBV DNA and a high barrier to viral resistance[3]. Entecavir, a new deoxyguanosine analog, represents a third agent within the nucleoside/nucleotide HBV polymerase inhibitor class with distinct advantages over lamivudine and adefovir dipivoxil: it has a three-step mechanism of action, is the most potent inhibitor of HBV DNA polymerase, is not associated with any major adverse effects, and has a limited potential for resistance. In phase II and III clinical trials, entecavir was found to be superior to lamivudine for all primary endpoints evaluated in both nucleoside-naïve and lamivudine-resistant patients. Entecavir was effective in both HBeAg-positive and HBeAg-negative nucleoside-naïve patients[4]. In chronic hepatitis B patients experiencing clevudine-induced myopathy, switching to entecavir 0.5 mg per day showed a resolution of myopathy and adequate viral suppression[5]. Entecavir (ETV) resistance of hepatitis B virus (HBV) conventionally requires rt184, 202, or 250 mutations plus lamivudine-resistance mutation (rtM204V/I ± L180M)[6].
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

3.39mL

0.68mL

0.34mL

16.93mL

3.39mL

1.69mL

33.86mL

6.77mL

3.39mL

参考文献

[1]Cheng JW, Merl MY, Nguyen HM. Effect of nesiritide on renal function: a retrospective review. Curr Med Res Opin. 2005 Nov;21(11):1857-63.

[2]Winter RW, Ignatushchenko M, et al. Potentiation of an antimalarial oxidant drug. Antimicrob Agents Chemother. 1997 Jul;41(7):1449-54.

[3]Rose RE, Hernandez D, Falk PJ, Ericson K, Zhou N, Thiry A, McPhee F. Discovery of the Novel Entecavir-Resistant Hepatitis B Virus Reverse Transcriptase A181C Substitution From an Integrated Genotypic Analysis. Hepatol Commun. 2018 Aug 21;2(9):1123-1135

[4]Rivkin A. A review of entecavir in the treatment of chronic hepatitis B infection. Curr Med Res Opin. 2005 Nov;21(11):1845-56

[5]Lee JW, Lee YJ, Lee JJ, Kim JH, Jung YK, Kwon OS, Choi DJ, Kim YS, Kim JH. [Efficacy of entecavir switching therapy in chronic hepatitis B patients with clevudine-induced myopathy]. Korean J Gastroenterol. 2013 Jan 25;61(1):30-6. Korean

[6]Liu Y, Zhou Y, Li X, Niu M, Chen R, Shao J, Si L, Luo D, Lin Y, Li L, Zhang K, Xiao X, Xu Z, Liu M, Lu M, Zoulim F, Xu D. Hepatitis B virus mutation pattern rtL180M+A181C+M204V may contribute to entecavir resistance in clinical practice. Emerg Microbes Infect. 2019;8(1):354-365