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CAS No.: 209216-23-9

恩替卡韦一水合物 Catalog No. CSN10912

Synonyms: BMS200475 monohydrate;SQ34676 monohydrate;SQ 34676

Entecavir, an analogue of guanosine, is reverse transcription inhibitor of HBV with EC50 of 3.75 nM in HepG2 cell.

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靶点选择性

生物活性

实验方案

技术信息

生物活性

靶点 HBV

EC50:3.75nM
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].
参考文献

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 3.3864 mL
- 16.9322 mL
- 33.8645 mL
- 5 mM
- 0.6773 mL
- 3.3864 mL
- 6.7729 mL
- 10 mM
- 0.3386 mL
- 1.6932 mL
- 3.3864 mL

技术信息

CAS号

209216-23-9

储存条件

粉末: Keep in dark place,Inert atmosphere,Room temperature

液体: -20°C:3-6 月 -80°C:12月

分子式

C12H17N5O4

运输

蓝冰

分子量

295.29

别名

BMS200475 monohydrate;SQ34676 monohydrate;SQ 34676;Entecavir Hydrate;Entecavir (hydrate);SQ 34,676;BMS-200475;BMS 200475-01;Baraclude;恩替卡韦 (1水合物)

溶解度

DMSO	59.0 mg/mL (199.8 mM)
Water	Insoluble
Ethanol	Insoluble

动物实验配方

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恩替卡韦一水合物 Catalog No. CSN10912