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エンテカビル

エンテカビル 化学構造式
142217-69-4
CAS番号.
142217-69-4
化学名:
エンテカビル
别名:
エンテカビル
英語化学名:
Entecavir
英語别名:
Etv;CS-863;CS-1236;Entecavi;SQ 34676;Enticavir;ENTECAVIR;Baraclude;entikawei;Aids098045
CBNumber:
CB0506719
化学式:
C12H15N5O3
分子量:
277.283
MOL File:
142217-69-4.mol

エンテカビル 物理性質

融点 :
249-252°C
沸点 :
661.4±65.0 °C(Predicted)
比重(密度) :
1.81±0.1 g/cm3(Predicted)
貯蔵温度 :
-20°C Freezer
外見 :
powder
酸解離定数(Pka):
14.22±0.60(Predicted)
色:
white to beige
光学活性 (optical activity):
[α]/D +25 to +40°, c = 0.2 in H2O
CAS データベース:
142217-69-4(CAS DataBase Reference)

安全性情報

Sフレーズ  24/25
WGK Germany  3
HSコード  29339900
有毒物質データの 142217-69-4(Hazardous Substances Data)

エンテカビル 価格 もっと(17)

メーカー 製品番号 製品説明 CAS番号 包装 価格 更新時間 購入
富士フイルム和光純薬株式会社(wako) W01COBQA-0464 エンテカビル
Entecavir
142217-69-4 250mg ¥43900 2018-12-26 購入
富士フイルム和光純薬株式会社(wako) W01COBQA-0464 エンテカビル
Entecavir
142217-69-4 100mg ¥25900 2018-12-26 購入
Sigma-Aldrich Japan SML1103 ≥98% (HPLC)
Entecavir ≥98% (HPLC)
142217-69-4 10mg ¥12000 2018-12-25 購入
Sigma-Aldrich Japan SML1103 ≥98% (HPLC)
Entecavir ≥98% (HPLC)
142217-69-4 50mg ¥48100 2018-12-25 購入
富士フイルム和光純薬株式会社(wako) W01TRCE558900 エンテカビル
Entecavir
142217-69-4 500mg ¥56300 2018-12-26 購入

エンテカビル 化学特性,用途語,生産方法

用途

抗ウイルス薬, 逆転写酵素阻害薬。

効能

抗ウイルス薬, 逆転写酵素阻害薬

説明

Entecavir is a cyclopentyl guanosine analog launched for the once-daily oral treatment of chronic hepatitis B virus (HBV) infection, and it is the third nucleoside or nucleotide analog to be marketed for this indication. Lamivudine, a deoxythiacytosine analog, and adefovir dipivoxil, a nucleotide analog, have been marketed since 1998 and 2002, respectively. Entecavir and adefovir are specifically indicated for HBV, whereas lamivudine is indicated for both HBV and HIV infections. In mammalian cells, entecavir is efficiently phosphorylated to the active triphosphate form, which competes with the natural substrate deoxyguanosine triphosphate and functionally inhibits all three activities of the HBV polymerase: (1) base priming, (2) reverse transcription of the negative strand from the pregenomic messenger RNA, and (3) synthesis of the positive strand of HBV DNA.The most common adverse events associated with the use of entecavir are similar to those typically seen with HBV therapy and include headache, abdominal pain, diarrhea, fatigue, and dizziness.

化学的特性

White to Off-White/Yellow Crystalline Powder

Originator

BMS (US)

使用

An oral antiviral drug used in the treatment of hepatitis B infection. A guanine analogue that inhhibits all three steps in the viral replication process

定義

ChEBI: Guanine substituted at the 9 position by a 4-hydroxy-3-(hydroxymethyl)-2-methylidenecyclopentyl group. A synthetic analogue of 2'-deoxyguanosine, it is a nucleoside reverse transcriptase inhibitor with selective antiviral activity against hepatitis B virus Entecavir is phosphorylated intracellularly to the active triphosphate form, which competes with deoxyguanosine triphosphate, the natural substrate of hepatitis B virus reverse transcriptase, inhibiting every stage of the enzyme's activity, although it ha no activity against HIV. It is used for the treatment of chronic hepatitis B.

brand name

Baraclude (Bristol-Myers Squibb).

応用例(製薬)

An analog of guanosine formulated as tablets and suspension for oral use.

薬物動態学

Oral absorption: 100%
Cmax 0.5 mg/kg oral: 4.2 ng/mL
Intracellular half-life: c. 16 h
Volume of distribution: In excess of body water
Plasma protein binding: 13%
Entecavir is rapidly absorbed after administration on an empty stomach, achieving peak plasma concentrations in 1–1.5 h. Plasma steady state is achieved in 6–10 days.
It is renally eliminated. Dosage adjustment is required with impaired creatinine clearance. The drug is not metabolized by cytochrome P450. No drug interactions have been identified.

臨床応用

Treatment of chronic hepatitis B virus infection in patients >16 years of age

副作用

Severity of adverse reactions was comparable to that of lamivudine, with headache, fatigue, upper respiratory infections and abdominal pain being most common. Lactic acidosis and hepatic steatosis were rarely observed.

エンテカビル 上流と下流の製品情報

原材料

準備製品


エンテカビル 生産企業

Global( 365)Suppliers
名前 電話番号 ファックス番号 電子メール 国籍 製品カタログ 優位度
Lianyungang happen teng technology co., LTD
15950718863
wang666xt@163.com CHINA 296 58
Beijing Yibai Biotechnology Co., Ltd
0086-182-6772-3597
sales04@yibaibiotech.com CHINA 420 58
Henan DaKen Chemical CO.,LTD.
+86-371-55531817
info@dakenchem.com CHINA 21836 58
Nanjing Gold Pharmaceutical Technology Co. Ltd.
025-84209270 15906146951
025-84209270 wgp@nanjing-pharmaceutical.com CHINA 115 55
Beijing Cooperate Pharmaceutical Co.,Ltd.
+86-10-60279497 +86(0)15646567669
+86-10-60279497 sales01@cooperate-pharm.com CHINA 1817 55
Henan Tianfu Chemical Co.,Ltd.
0371-55170693
0371-55170693 info@tianfuchem.com CHINA 22625 55
PI & PI BIOTECH INC.
18371201331
020-81716319 Sales@pipitech.com CHINA 3048 55
Shanghai Yingrui Biopharma Co., Ltd.
+86-21-33585366 E-mail:sales03@shyrchem.com
+86-21-34979012 sales03@shyrchem.com CHINA 739 60
ATK CHEMICAL COMPANY LIMITED
+86 21 5161 9050/ 5187 7795
+86 21 5161 9052/ 5187 7796 ivan@atkchemical.com CHINA 24754 60
Hebei Minshang Biotechnology Co., Ltd
+86-13582176207 +86-13582176207
cathy@hbminshang.cn CHINA 312 58

142217-69-4(エンテカビル)キーワード:


  • 142217-69-4
  • Aids098045
  • Aids-098045
  • Etv
  • EntikaweiPian
  • 2-Amino-9-((1S,3R,4S)-4-hydroxy-3-(hydroxymethyl)-2-methylenecyclopentyl)-3H-purin-6(9H)-one ,99.7%
  • Enticavir
  • (1S,3R,4S)-9-[4-Hydroxy-3-(hydroxyMethyl)-2-Methylenecyclopentyl]guanine
  • Entecavir Anhydrous
  • 20MG/100MG/100G
  • Entecavir Tablets
  • 2-amino-9-((1S,3R,4S)-4-hydroxy-3-(hydroxymethyl)-2-methylenecyclopentyl)-1H-purin-6(9H)-one
  • Entecavir USP Impurity B
  • Entecavir/Entecavir Monohydrate
  • Entecavir (as hydrate)
  • Entecavir,99%e.e.
  • ENTECAVIR
  • Entecavi
  • ENTECAVIR, 98-102%
  • entecavir Baraclude
  • 2-Amino-9-[4-hydroxy-3-(hydroxymethyl)-2-methylidene-cyclopentyl]-3H-purin-6-one, Baraclude
  • 2-Amino-9-[4-hydroxy-3-(hydroxymethyl)-2-methylidene-cyclopentyl]-3H-purin-6-one
  • Baraclude
  • SQ 34676
  • 6-H-Purin-6-one-,2-amino-1,9-dihydro-9-[(1S,3R,4S)-4-hydroxy-3-(hydroxymethyl)-2-methylenecyclopentyl]
  • CS-1236
  • Entecavir, BMS200475
  • 2-amino-9-[(1R,3R,4S)-4-hydroxy-3-(hydroxymethyl)-2-methylenecyclopentyl]-3H-purin-6-one hydrate
  • CS-863
  • entikawei
  • Entecavir(SQ 34676
  • エンテカビル
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