ChemicalBook
Chinese english Germany

テノホビル水和物

テノホビル水和物 化学構造式
147127-20-6
CAS番号.
147127-20-6
化学名:
テノホビル水和物
别名:
テノホビル水和物;(R)-[[2-(6-アミノ-9H-プリン-9-イル)-1-メチルエトキシ]メチル]ホスホン酸水和物;テノホビル
英語化学名:
Tenofovir
英語别名:
Viread;9-Pmpa;GS-1278;GS 1275;(R)-PMPA;Tenofovi;TENOFOVIR;Tenefovir;Apropovir;Aids021800
CBNumber:
CB8218508
分子式:
C9H14N5O4P
分子量:
287.21
MOL File:
147127-20-6.mol

テノホビル水和物 物理性質

融点 :
276-280°C
比旋光度 :
D +21° (c = 1 in 0.1M HCl)
貯蔵温度 :
Store at -20°C
外見 :
powder
色:
white to beige
光学活性 (optical activity):
[α]/D -20 to -26°, c = 0.5 in 1 M HCl
水溶解度 :
13.4 mg/mL (25 ºC)
Merck :
14,9146
CAS データベース:
147127-20-6(CAS DataBase Reference)

安全性情報

RTECS 番号 SZ6563600
HSコード  29339900

テノホビル水和物 価格 もっと(8)

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) W01TOC3666
Tenofovir
147127-20-6 10mg ¥41000 2018-12-26 購入
富士フイルム和光純薬株式会社(wako) W01TOC3666
Tenofovir
147127-20-6 50mg ¥184000 2018-12-26 購入
東京化成工業 T3006 テノホビル水和物 >98.0%(HPLC)(T)
Tenofovir Hydrate >98.0%(HPLC)(T)
147127-20-6 1g ¥6600 2018-12-04 購入
東京化成工業 T3006 テノホビル水和物 >98.0%(HPLC)(T)
Tenofovir Hydrate >98.0%(HPLC)(T)
147127-20-6 5g ¥23100 2018-12-04 購入
Sigma-Aldrich Japan SML1795 ≥98% (HPLC)
Tenofovir ≥98% (HPLC)
147127-20-6 5mg ¥21000 2018-12-25 購入

テノホビル水和物 化学特性,用途語,生産方法

用途

テノホビル(Tenofovir、テノフォビルとも)は抗ウイルス薬の一つ。ジソプロキシルエステルまたはアラフェナミド(アラニンイソプロピルエステルとのアミド+フェノールとのエステル)のフマル酸塩として販売されている。 HIV感染症やB型肝炎の治療に用いられる。

用途

DNA ポリメラーゼによる基質 取り組みを競合的に阻害し、DNA 鎖の伸長停 止作用を示します。

化学的特性

White Crystalline Solid

使用

Tenofovir is a drug used for the treatment of chronic heptatitis B as well as prevention and treatment of HIV/AIDS. It is a kind of nucleotide analog, acting as the reverse-transcriptase inhibitor (NtRTI). It inhibits the activity of HIV reverse transcriptase through competing with the natural substrate deoxyadenosine 5’-triphosphate, causing the termination of DNA chain. 

定義

ChEBI: A member of the class of phosphonic acids that is methylphosphonic acid in which one of the methyl hydrogens is replaced by a [(2R)-1-(6-amino-9H-purin-9-yl)propan-2-yl]oxy group. An inhibitor of HIV-1 reverse transcriptase, the bis(isopropyloxycarbonyloxy ethyl) ester (disoproxil ester) prodrug is used as the fumaric acid salt in combination therapy for the treatment of HIV infection.

獲得抵抗性

HIV variants with the K65R mutation and the K70E mutation in the reverse transcriptase demonstrate reduced susceptibility to tenofovir.

応用例(製薬)

A nucleotide analog structurally similar to adefovir.
EC50 values for HBV, assessed in the HepG2 2.2.15 cell line, ranged from 0.14 to 1.5 μm; the cytotoxic concentration exceeded 100 μm. A decline in HBV DNA levels below 105 copies/mL at 48 weeks of therapy in 100% of patients receiving tenofovir compared with 44% on adefovir therapy has been reported. There are also case reports of patients with primary resistance to adefovir responding to tenofovir.
It is generally well tolerated in patients with chronic HBV; the most common side effects include nausea and gastrointestinal upset, headache, dizziness, fatigue and rash.

応用例(製薬)

An acyclic nucleoside phosphonate, formulated as the disoproxil fumarate salt for oral administration.

生物活性

Selectively inhibits HIV reverse transcriptase (RNA-dependent DNA polymerase). Prevents cytotoxicity in SIV-infected C-8166 cells in vitro (IC 50 = 1.5 μ M). Antiviral agent.

薬物動態学

Oral absorption: c. 25%
Cmax 300 mg once daily: 0.3 mg/L
Plasma half-life: 17 h
Volume of distribution: 1.3 ± 0.6 L/kg at 3.0 mg/kg intravenous dose
Plasma protein binding: <0.7% (in vitro)
Absorption and distribution
Oral bioavailability is poor, but is enhanced by administration as the disoproxil prodrug. It may be taken with or without food. CSF penetration is likely to be minimal due to the anionic charge of the molecule at physiological pH. It accumulates in semen at higher concentrations than in plasma. It is not known if it is distributed into breast milk.
Metabolism and excretion
Tenofovir is not metabolized and is principally eliminated by the kidneys by a combination of glomerular filtration and active tubular secretion. In patients with renal dysfunction the dose should be adjusted accordingly.
Compounds such as cidofovir, aciclovir (acyclovir), valaciclovir, ganciclovir, valganciclovir and probenecid may compete for renal excretion. Tenofovir levels are increased when prescribed with some HIV protease inhibitors. The co-administration of tenofovir with didanosine leads to didanosine accumulation which is thought to occur through inhibition of purine nucleoside phosphorylase. This has been associated with impaired immune recovery and several cases of lactic acidosis and pancreatitis. If tenofovir is combined with didanosine the dose of didanosine should be reduced to 200 mg (<60 kg) or 250 mg (≥60 kg) per day and the patient monitored for symptoms of didanosine toxicity.

臨床応用

Chronic hepatitis B infection

臨床応用

Treatment of HIV infection in adults and children (in combination with other antiretroviral drugs)

副作用

In clinical trials of antiretroviral treatment-naive participants, the most commonly reported adverse events were mild to moderate gastrointestinal upset (nausea 8%, diarrhea 11%), headache (14%) and depression (11%). Tenofovir has the potential to result in nephrotoxicity, particularly through proximal tubular damage, but the risk of clinically significant renal dysfunction appears relatively low and seems to occur mainly in subjects with other identifiable risks for renal impairment. Minor elevations in serum creatinine and reductions in creatinine clearance occur, but rarely require drug discontinuation.
A few (<0.1%) cases of osteomalacia and decreased bone density have been reported.

テノホビル水和物 上流と下流の製品情報

原材料

準備製品


テノホビル水和物 生産企業

Global( 366)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
Shanghai Yingrui Biopharma Co., Ltd.
+86-21-33585366 E-mail:sales03@shyrchem.com
+86-21-34979012 sales03@shyrchem.com CHINA 663 60
Capot Chemical Co.,Ltd.
+86 (0)571-855 867 18
+86 (0)571-858 647 95 sales@capotchem.com China 19953 60
Shenzhen Sendi Biotechnology Co.Ltd.
0755-23311925 18102838259
0755-23311925 Abel@chembj.com CHINA 3217 55
Henan DaKen Chemical CO.,LTD.
+86-371-55531817
info@dakenchem.com CHINA 22049 58
Nanjing Gold Pharmaceutical Technology Co. Ltd.
025-84209270 15906146951
025-84209270 wgp@nanjing-pharmaceutical.com CHINA 117 55
Beijing Cooperate Pharmaceutical Co.,Ltd.
+86-10-60279497 +86(0)15646567669
+86-10-60279497 sales01@cooperate-pharm.com CHINA 1530 55
Henan Tianfu Chemical Co.,Ltd.
0371-55170693
0371-55170693 info@tianfuchem.com CHINA 20786 55
Mainchem Co., Ltd.
+86-0592-6210733
+86-0592-6210733 sales@mainchem.com CHINA 32651 55
ATK CHEMICAL COMPANY LIMITED
+86 21 5161 9050/ 5187 7795
+86 21 5161 9052/ 5187 7796 ivan@atkchemical.com CHINA 14293 60
Hubei Jusheng Technology Co.,Ltd.
86-155-27864001
peter@hubeijusheng.com CHINA 18004 58

147127-20-6(テノホビル水和物)キーワード:


  • 147127-20-6
  • (R)-(1-(6-aMino-9H-purin-9-yl)propan-2-yloxy)Methylphosphonic acid
  • Tenofovir (PMPA)
  • Tenofovir(Viread)
  • [[(1R)-2(6-AMino-9H-purin-9-yl)-1-Methylethoxy]Methyl]ph
  • Viread
  • 1-(6-AMinopurin-9-yl)propan-2-yloxyMethylphosphonic acid(PMPA)
  • Tenofovir 1-(6-Aminopurin-9-yl)propan-2-yloxymethylphosphonic acid
  • R-PMPA, Tenofovir,
  • Tenofovir, >=98%
  • Tenofovir free base
  • (((1-(6-Amino-9H-purin-9-yl)propan-2-yl)oxy)methyl)phosphonic acid
  • (R)-(((1-(6-AMINO-9H-PURIN-9-YL)PROPAN-2-YL)OXY)METHYL)PHOSPHONIC
  • tenofovir (anhydrous)
  • Tenofovirdisoproxil Intermediate PMPA
  • 1-(6-aminopurin-9-yl)propan-2-yloxymethylphosphonic acid
  • D,L-TENOFOVIR
  • TENOFOVIR
  • (R)-9-(2-PHOSPHONYLMETHOXYPROPYL)-ADENINE
  • (R)-9-(2-Phosphonomethoxypropyl)Adenine
  • Tenofovir(ForResearchOnly)
  • (R)-PMPA
  • [[(1R)-2(6-Amino-9H-purin-9-yl)-1-methylethoxy]methyl]phosphonic Acid
  • GS-1278
  • Tenofovir disoproxil fumarate and intermediates
  • (R)-9-[2-(Phosphonomethoxy)propyl]adenine (PMPA)
  • GS 1275
  • Phosphonic acid, [[(1R)-2-(6-amino-9H-purin-9-yl)-1-methylethoxy]methyl]- (9CI)
  • Phosphonic acid, [[2-(6-amino-9H-purin-9-yl)-1-methylethoxy]methyl]-, (R)-
  • Tenofovi
  • Tenofovir Disoproxil Fumarate impurity P
  • テノホビル水和物
  • (R)-[[2-(6-アミノ-9H-プリン-9-イル)-1-メチルエトキシ]メチル]ホスホン酸水和物
  • テノホビル
Copyright 2017 © ChemicalBook. All rights reserved