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ポサコナゾール

ポサコナゾール 化学構造式
171228-49-2
CAS番号.
171228-49-2
化学名:
ポサコナゾール
别名:
ポサコナゾール
英語化学名:
Posaconazole
英語别名:
Pcz;Pos;Noxafil;Sch 56592;EOS-60773;Aids058495;Aids-058495;Posconazole;Posaconazole;posaconazote
CBNumber:
CB9946972
化学式:
C37H42F2N8O4
分子量:
700.78
MOL File:
171228-49-2.mol

ポサコナゾール 物理性質

融点 :
170-1720C
闪点 :
9℃
貯蔵温度 :
-20°C Freezer
外見 :
powder
色:
white to beige
光学活性 (optical activity):
[α]/D -24 to -32°, c = 1.0 in chloroform-d
Merck :
14,7602
InChIKey:
RAGOYPUPXAKGKH-XAKZXMRKSA-N
CAS データベース:
171228-49-2(CAS DataBase Reference)
安全性情報
  • リスクと安全性に関する声明
  • 危険有害性情報のコード(GHS)
主な危険性  F,T
Rフレーズ  11-23/24/25-39/23/24/25
Sフレーズ  7-16-36/37-45
RIDADR  UN1230 - class 3 - PG 2 - Methanol, solution
WGK Germany  3
RTECS 番号 XZ5481020
有毒物質データの 171228-49-2(Hazardous Substances Data)
絵表示(GHS)
注意喚起語 Danger
危険有害性情報
コード 危険有害性情報 危険有害性クラス 区分 注意喚起語 シンボル P コード
H225 引火性の高い液体および蒸気 引火性液体 2 危険 P210,P233, P240, P241, P242, P243,P280, P303+ P361+P353, P370+P378,P403+P235, P501
H370 臓器の障害 特定標的臓器有害性、単回暴露 1 危険 P260, P264, P270, P307+P311, P321,P405, P501
注意書き
P210 熱/火花/裸火/高温のもののような着火源から遠ざ けること。-禁煙。
P260 粉じん/煙/ガス/ミスト/蒸気/スプレーを吸入しないこ と。
P280 保護手袋/保護衣/保護眼鏡/保護面を着用するこ と。
P301+P310 飲み込んだ場合:直ちに医師に連絡すること。
P311 医師に連絡すること。

ポサコナゾール 価格 もっと(10)

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) W01TRCP689600 ポサコナゾール
Posaconazole
171228-49-2 1mg ¥12500 2018-12-26 購入
富士フイルム和光純薬株式会社(wako) W01MAS125220 ポサコナゾール
Posaconazole
171228-49-2 1g ¥261400 2018-12-26 購入
東京化成工業 P2477 ポサコナゾール >98.0%(HPLC)
Posaconazole >98.0%(HPLC)
171228-49-2 10mg ¥10900 2018-12-04 購入
東京化成工業 P2477 ポサコナゾール >98.0%(HPLC)
Posaconazole >98.0%(HPLC)
171228-49-2 50mg ¥32800 2018-12-04 購入
Sigma-Aldrich Japan P-103 2.0?mg/mL in methanol, ampule of 1?mL, certified reference material
Posaconazole solution 2.0?mg/mL in methanol, ampule of 1?mL, certified reference material
171228-49-2 1ml ¥31600 2018-12-25 購入

ポサコナゾール 化学特性,用途語,生産方法

化学的特性

White Solid

使用

Orally active triazole antifungal.

使用

Posaconazole is a sterol C14ɑ demethylase inhibitor with an IC50 of 0.25 nM

定義

ChEBI: An N-arylpiperazine that consists of piperazine carrying two 4-substituted phenyl groups at positions 1 and 4. A triazole antifungal drug.

抗菌性

The spectrum includes dimorphic fungi (Blast. dermatitidis, Coccidioides spp., Hist. capsulatum, Pen. marneffei, and Spor. schenckii), molds (Aspergillus spp., Mucor spp., Rhizomucor spp. and Rhizopus spp.), some dematiaceous fungi and yeasts (Candida spp. and Cryptococcus spp.).

一般的な説明

Technetium (99mTc) exametazime is a mixture of unstablelipophilic enantiomers that rapidly cross the blood-brain barrierand is trapped in the tissues. The proposed trapping mechanismfor localization includes reduction by glutathione. Asimilar diffusion and trapping process occurs with autologouslymphocytes in vitro.
Exametazime is also known as hexamethylpropyleneamineoxime or HMPAO. The radiolabeled complex is indicated for cerebral perfusion in stroke, but is most commonlyused for the radiolabeling of autologous leukocytesas an adjunct in the localization of intra-abdominal infectionand inflammatory bowel disease.
Each kit includes several components: (a) reaction vialscontaining a mixture of exametazime, stannous chloride,and sodium chloride; (b) vials of 1% methylene blue; (c)vials of phosphate buffer in 0.9% NaCl; and (d) 0.45-μm syringefilters. Product preparation depends on the intendeduse.

応用例(製薬)

A synthetic triazole available for oral administration.

薬物動態学

Cmax 200 mg oral: 0.5 mg/L after 4 h
Plasma half-life: 35 h
Volume of distribution: 1774 L
Plasma protein binding: >98%
Absorption
Oral absorption is slow. Absorption from the gastrointestinal tract is improved if the drug is given with a high-fat meal. Blood concentrations increase in proportion to dosage up to 800 mg.
Distribution
It is extensively distributed into body tissues.
Metabolism and excretion
It is not as extensively metabolized by the hepatic cytochrome P450 system as other triazole antifungals. More than 70% of an administered dose is eliminated in the feces, predominantly as unchanged drug. The remainder is excreted as glucuronidated derivatives in the urine. Posaconazole is a substrate for intestinal P-glycoprotein,an adenosine triphosphate-dependent plasma membrane transporter responsible for drug efflux from cells. Multiple peaks in blood concentrations have been observed, suggesting that effluxed drug is reabsorbed into the systemic circulation.

臨床応用

Invasive aspergillosis
Fusarium infection
Chromoblastomycosis and mycetoma
Coccidioidomycosis
Oropharyngeal candidosis
Prophylaxis of invasive fungal infections in patients at serious risk
With the exception of oropharyngeal candidosis and prophylaxis, use is presently restricted to patients with disease that is refractory to other antifungal drugs, or who are intolerant to them.

副作用

It is generally well tolerated even for long periods. Unwanted effects include gastrointestinal discomfort and mild to moderate, transient abnormalities of liver enzymes. Rare side effects include cholestasis and hepatic failure.

ポサコナゾール 上流と下流の製品情報

原材料

準備製品


ポサコナゾール 生産企業

Global( 281)Suppliers
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171228-49-2(ポサコナゾール)キーワード:


  • 171228-49-2
  • 4-(4-(4-(4-(((3R,5R)-5-((1H-1,2,4-triazol-1-yl)methyl)-5-(2,4-difluorophenyl)tetrahydrofuran-3-yl)methoxy)phenyl)piperazin-1-yl)phenyl)-2-((2S,3S)-2-hydroxypentan-3-yl)-2,4-dihydro-3H-1,2,4-triazol-3-one
  • 4-(4-(4-(4-(((3R,5R)-5-((1H-1,2,4-Triazol-1-yl)methyl)-5-(2,4-difluorobenzyl)tetrahydrofuran-3
  • Posaconazole(Form Ⅲ)
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  • 2,5-Anhydro-1,3,4-trideoxy-2-C-(2,4-difluorophenyl)-4-[[4-[4-[4-[1-[(1S,2S)-1-ethyl-2-hydroxypropyl]-1,5-dihydro-5-oxo-4H-1,2,4-triazol-4-yl]phenyl]-1-piperazinyl]phenoxy]methyl]-1-(1H-1,2,4-triazol-1-yl)-D-threo-pentitol
  • Noxafil
  • Sch 56592
  • 4-[4-[4-[4-[[(3R,5R)-5-(2,4-Difluorophenyl)-5-(1,2,4-triazol-1-ylmethyl)oxolan-3-yl]methoxy]phenyl]piperazin-1-yl]phenyl]-2-[(2S,3S)-2-hydroxypentan-3-yl]-1,2,4-triazol-3-one
  • HYDROXYPROPYL]-2,4-DIHYDRO-3H-1,2,4-TRIAZOL-3-ONE
  • Posaconazole for research
  • 1-((1S,2S)-1-Ethyl-2-hydroxypropyl)-4-{4-[4-(4-{[(5S,3R)-5-(2,4-difluorophenyl)-5-(1,2,4-triazolylmethyl)oxolan-3-yl]methoxy}phenyl)piperazinyl]phenyl}-1,2,4-triazolin-5-one
  • Aids058495
  • Aids-058495
  • POSACONAZOLE whatsapp
  • EOS-60773
  • posaconazote
  • Posaconazole and intermediates
  • Posaconazole(Form Ⅰ)
  • Pcz
  • Pos
  • Posconazole
  • 4-{4-[4-(4-{[(3S,5R)-5-(2,4-difluorophenyl)-5-(1H-1,2,4-triazol-1-ylMethyl)oxolan-3-yl]Methoxy}phenyl)piperazin-1-yl]phenyl}-1-[(2S,3S)-2-hydroxypentan-3-yl]-4,5-dihydro-1H-1,2,4-triazol-5-one
  • 4-(4-(4-(4-(((3R,5R)-5-(3,4-difluorophenyl)-5-(1H-1,2,4-triazol-1-yl)tetrahydrofuran-3-yl)Methoxy)phenyl)piperazin-1-yl)phenyl)-1-((2S,3S)-2-hydroxypentan-3-yl)-1H-1,2,4-triazol-5(4H)-one
  • Pasaconazole
  • 4-(4-(4-(4-(((3R,5R)-5-((1H-1,2,4-Triazol-1-yl)Methyl)-5-(2,4-difluorophenyl)tetrahydrofuran-3-yl)Methoxy)phenyl)piperazin-1-yl)phenyl)-1-((2S,3S)-2-hydroxypentan-3-yl)-1H-1,2,4-triazol-5(4H)-one
  • D-threo-Pentitol,2,5-anhydro-1,3,4-trideoxy-2-C-(2,4-difluorophenyl)-4-[[4-[4-[4-[1-[(1S,2S)-1-ethyl-2-hydroxypropyl]-1,5-dihydro-5-oxo-4H-1,2,4-triazol-4-yl]phenyl]-1-piperazinyl]phenoxy]Methyl]-1-(1H-1,2,4-triazol-1-yl)-
  • 4-(4-(4-(4-(((3R,5R)-5-((1H-1,2,4-triazol-1-yl)methyl)-5-(2,4-difluorophenyl)-tetrahydrofuran-3-yl)methoxy)phenyl)piperazin-1-yl)phenyl)-2-((2S,3S)-2-hydroxypentan-3-yl)-2H-1,2,4-triazol-3(4H)-one
  • Posaconazole 4-[4-[4-[4-[[(3R,5R)-5-(2,4-Difluorophenyl)-5-(1,2,4-triazol-1-ylmethyl)oxolan-3-yl]methoxy]phenyl]piperazin-1-yl]phenyl]-2-[(2S,3S)-2-hydroxypentan-3-yl]-1,2,4-triazol-3-one
  • Posaconazole solution
  • Posaconazole Amorphous
  • ポサコナゾール
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