恩替卡韦

恩替卡韦结构式
恩替卡韦
常用名 恩替卡韦 英文名 Entecavir
CAS号 142217-69-4 分子量 277.279
密度 1.8±0.1 g/cm3 沸点 734.2ºC at 760 mmHg
分子式 C12H15N5O3 熔点 249-252ºC
MSDS恩替卡韦的MSDS|SDS|pdf下载 美版 闪点 397.9ºC

 恩替卡韦用途


为鸟嘌呤核苷类似物,对乙肝病毒(HBV)多聚酶具有抑制作用。

 恩替卡韦作用


本品为鸟嘌呤核苷类似物,对乙肝病毒(HBV)多聚酶具有抑制作用。它能够通过磷酸化成为具有活性的三磷酸盐,三磷酸盐在细胞内的半衰期为15小时。通过与HBV多聚酶的天然底物三磷酸脱氧鸟嘌呤核苷竞争,恩替卡韦三磷酸盐能抑制病毒多聚酶(逆转录酶)的所有三种活性:(1)HBV多聚酶的启动;(2)前基因组mRNA逆转录负链的形成;(3)HBV DNA正链的合成。恩替卡韦三磷酸盐对HBV DNA多聚酶的抑制常数(Ki)为0.0012μM。恩替卡韦三磷酸盐对细胞的α、β、δDNA多聚酶和线粒体γDNA多聚酶抑制作用较弱,Ki值为18至于160μM。

 恩替卡韦物理化学性质

[ 密度 ]: 1.8±0.1 g/cm3
[ 沸点 ]: 734.2ºC at 760 mmHg
[ 熔点 ]: 249-252ºC
[ 分子式 ]: C12H15N5O3
[ 分子量 ]: 277.279
[ 闪点 ]: 397.9ºC
[ 精确质量 ]: 277.117493
[ PSA ]: 130.05000
[ LogP ]: -0.96
[ 外观性状 ]: 白色至灰白色/黄色结晶粉末
[ 折射率 ]: 1.837

 恩替卡韦MSDS

 恩替卡韦安全信息

[ 危险品运输编码 ]: NONH for all modes of transport
[ 海关编码 ]: 2933990090

 恩替卡韦合成线路

 恩替卡韦海关

[ 海关编码 ]: 2933990090
[ 中文概述 ]: 2933990090. 其他仅含氮杂原子的杂环化合物. 增值税率:17.0%. 退税率:13.0%. 监管条件:无. 最惠国关税:6.5%. 普通关税:20.0%
[申报要素 ]: 品名, 成分含量, 用途, 乌洛托品请注明外观, 6-己内酰胺请注明外观, 签约日期
[ Summary ]: 2933990090. heterocyclic compounds with nitrogen hetero-atom(s) only. VAT:17.0%. Tax rebate rate:13.0%. . MFN tariff:6.5%. General tariff:20.0%

 恩替卡韦文献18

更多文献
Formation of covalently closed circular DNA in Hep38.7-Tet cells, a tetracycline inducible hepatitis B virus expression cell line.

Biochem. Biophys. Res. Commun. 452(3) , 315-21, (2014)

Hepatitis B virus (HBV) covalently closed circular DNA (cccDNA) plays a central role in chronic HBV infection. However, analysis of the molecular mechanism of cccDNA formation is difficult because of ...

Influence of the basal core promoter and precore mutation on replication of hepatitis B virus and antiviral susceptibility of different genotypes.

J. Med. Virol. 87(4) , 601-8, (2015)

Mutations in the basal core promoter (BCP) and precore (PC) regions of the hepatitis B virus (HBV) are more common in genotypes B and C than in genotype A, suggesting that these mutations might affect...

Decreased liver distribution of entecavir is related to down-regulation of Oat2/Oct1 and up-regulation of Mrp1/2/3/5 in rat liver fibrosis.

Eur. J. Pharm. Sci. 71 , 73-9, (2015)

We aimed to elucidate whether entecavir was taken-up into liver by transporters and clarify the possible molecular mechanisms of changes in the distribution of entecavir in rat liver fibrosis.Thioacet...

 恩替卡韦英文别名

2-Amino-9-[(1S,3R,4S)-4-hydroxy-3-(hydroxymethyl)-2-methylenecyclopentyl]-1,9-dihydro-6H-purin-6-one
entecavir (anhydrous)
6H-Purin-6-one, 2-amino-1,9-dihydro-9-((1S,3R,4S)-4-hydroxy-3-(hydroxymethyl)-2-methylenecyclopentyl)-
2-amino-9-[(1S,3R,4S)-4-hydroxy-3-(hydroxymethyl)-2-methylidenecyclopentyl]-3H-purin-6-one
2-amino-9-[(1S,3R,4S)-4-hydroxy-3-(hydroxymethyl)-2-methylidenecyclopentyl]-1,9-dihydro-6H-purin-6-one
6H-Purin-6-one, 2-amino-1,9-dihydro-9-[(1S,3R,4S)-4-hydroxy-3-(hydroxymethyl)-2-methylenecyclopentyl]-
Baraclude
entecavir
9H-purin-6-ol, 2-amino-9-[(1S,3R,4S)-4-hydroxy-3-(hydroxymethyl)-2-methylenecyclopentyl]-
UNII-NNU2O4609D
2-amino-9-[(1S,3R,4S)-4-hydroxy-3-(hydroxymethyl)-2-methylidenecyclopentyl]-9H-purin-6-ol
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参考价格:¥468/100mg

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