カスポファンギン

カスポファンギン 化学構造式
162808-62-0
CAS番号.
162808-62-0
化学名:
カスポファンギン
别名:
カスポファンギン;カスポファンジン;シクロ[L-Thr-4β-ヒドロキシ-L-Pro-[(4S)-4-ヒドロキシ-4-(4-ヒドロキシフェニル)-L-Thr-]-[(3R)-3-ヒドロキシ-L-Orn-]-3β-ヒドロキシ-L-Pro-[(4R,5S)-N2-[(10R,12S)-10,12-ジメチルテトラデカノイル]-4-ヒドロキシ-5-(2-アミノエチルアミノ)-L-Orn*-]];カスポフンギン;シクロ[L-Thr-L-t4Hyp-[(3S,4S)-3,4-ジヒドロキシ-4-(4-ヒドロキシフェニル)-L-Abu-]-[(3R)-3-ヒドロキシ-L-Orn-]-[(3S)-3-ヒドロキシ-L-Pro-]-[(4R,5S)-5-[(2-アミノエチル)アミノ]-4-ヒドロキシ-N2-[(10R,12S)-10,12-ジメチル-1-オキソテトラデシル]-L-Orn*-]];(10R,12S)-N-[(3S,6S,9S,11R,15S,18S,20R,21S,24S,25S)-3-[(1R)-3-アミノ-1-ヒドロキシプロピル]-21-[(2-アミノエチル)アミノ]-6-[(1S,2S)-1,2-ジヒドロキシ-2-(4-ヒドロキシフェニル)エチル]-11,20,25-トリヒドロキシ-15-[(1R)-1-ヒドロキシエチル]-2,5,8,14,17,23-ヘキサオキソ-1,4,7,13,16,22-ヘキサアザトリシクロ[22.3.0.09,13]ヘプタコサン-18-イル]-10,12-ジメチルテトラデカンアミド;キャスポファンギン
英語名:
Caspofungin
英語别名:
Caspofungine;Caspofungin (Base);m991;CS-1171;Aids058650;Aids-058650;CASPOFUNGIN;CASPORFUNGIN;Cancidas (tm);Caspofungin MK-0991
CBNumber:
CB91073222
化学式:
C52H88N10O15
分子量:
1093.31
MOL File:
162808-62-0.mol

カスポファンギン 物理性質

沸点 :
1408.1±65.0 °C(Predicted)
比重(密度) :
1.36±0.1 g/cm3(Predicted)
酸解離定数(Pka):
9.86±0.26(Predicted)

安全性情報

有毒物質データの 162808-62-0(Hazardous Substances Data)

カスポファンギン 価格

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

カスポファンギン 化学特性,用途語,生産方法

効能

抗真菌薬, 細胞壁合成阻害薬

使用

Caspofungin is an antifungal drug, and belongs to a new class termed the echinocandins. It is used to treat Aspergillus and Candida infection, and works by inhibiting cell wall synthesis. Antifungals in the echinocandin class inhibit the synthesis of glucan in the cell wall, probably via the enzyme 1,3-beta glucan synthase. There is a potential for resistance development to occur, however in vitro resistance development to Caspofungin by Aspergillus species has not been studied.

定義

ChEBI: A semisynthetic cyclic hexapeptide echinocandin antibiotic which exerts its effect by inhibiting the synthesis of 1,3-beta-D-glucan, an integral component of the fungal cell wall.

抗菌性

It is active against Aspergillus spp., Candida spp. and the cyst form of Pn. jirovecii.

獲得抵抗性

This is rare, but resistant strains of C. albicans, C. glabrata and C. parapsilosis have been recovered from patients failing caspofungin treatment. These strains are typically cross-resistant to other echinocandins.

応用例(製薬)

A semisynthetic lipopeptide derived from a fermentation product of Glarea lozoyensis. Formulated as the diacetate for intravenous infusion.

作用機序

Caspofungin inhibits the synthesis of beta-(1,3)-D-glucan, an essential component of the cell wall of Aspergillus species and Candida species. beta-(1,3)-D-glucan is not present in mammalian cells. The primary target is beta-(1,3)-glucan synthase.

薬物動態学

Cmax 70 mg 1-h infusion: c. 10 mg/L 1 h post infusion
Plasma half-life: 9–11 h
Volume of distribution: 0.15 L/kg
Plasma protein binding: 97%
Blood concentrations increase in proportion to dosage.
Distribution
The drug is widely distributed, the highest concentrations being found in the liver. Levels in the CSF are negligible.
Metabolism and excretion
It is slowly metabolized by the liver through non-enzymatic peptide hydrolysis and N-acetylation, and the two inactive metabolites are excreted in the feces and bile. No dosage adjustment is required in patients with renal impairment; however, a dose reduction to 35 mg following the 70 mg loading dose is recommended for patients with moderate hepatic impairment. Caspofungin is not cleared by hemodialysis.

臨床応用

Candidemia and certain invasive forms of candidosis
Esophageal candidosis
Invasive aspergillosis unresponsive to other antifungal drugs
Empirical treatment of presumed fungal infections in febrile neutropenic patients

副作用

Occasional histamine-mediated infusion-related reactions, injection site reactions and transient abnormalities of liver enzymes have been reported. Rare cases of significant hepatic dysfunction, hepatitis or worsening liver failure have also been described.

カスポファンギン 上流と下流の製品情報

原材料

準備製品


カスポファンギン 生産企業

Global( 140)Suppliers
名前 電話番号 電子メール 国籍 製品カタログ 優位度
AFINE CHEMICALS LIMITED
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+86-0371-55170693 +86-19937530512
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+86-592-6051114 +8618959220845
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Baoji Guokang Healthchem co.,ltd
+8615604608665 15604608665
dominicguo@gk-bio.com CHINA 9427 58

カスポファンギン  スペクトルデータ(1HNMR)


162808-62-0(カスポファンギン)キーワード:


  • 162808-62-0
  • CASPOFUNGIN
  • CASPORFUNGIN
  • PneuMocandin B0,1-[(4R,5S)-5-[(2-aMinoethyl)aMino]-N2-(10,12-diMethyl-1-oxotetradecyl)-4-hydroxy-L-ornithine]-5-[(3R)-3-hydroxy-L-ornithine]-
  • Aids058650
  • Aids-058650
  • Cancidas (tm)
  • m991
  • Caspofungin .CH3COOH
  • (10R,12R)-N-[(3S,6S,9S,11R,15S,18S,20R,21S,24S,25S)-3-[(1R)-3-aMino-1-hydroxypropyl]-21-[(2-aMinoethyl)aMino]-6-[(1S,2S)-1,2-dihydroxy-2-(4-hydroxyphenyl)ethyl]-11,20,25-trihydroxy-15-[(1R)-1-hydroxyethyl]-2,5,8,14,17,23-hexaoxo-1,4,7,13,16,22-hexaazatric
  • CS-1171
  • Caspofungin MK-0991
  • Pneumocandin B0, 1-[(4R,5S)-5-[(2-aminoethyl)amino]-N2-[(10R,12S)-10,12-dimethyl-1-oxotetradecyl]-4-hydroxy-L-ornithine]-5-[(3R)-3-hydroxy-L-ornithine]-
  • Caspofungin USP/EP/BP
  • Caspofungin diformate salt
  • Caspofungine
  • Caspofungin (Base)
  • カスポファンギン
  • カスポファンジン
  • シクロ[L-Thr-4β-ヒドロキシ-L-Pro-[(4S)-4-ヒドロキシ-4-(4-ヒドロキシフェニル)-L-Thr-]-[(3R)-3-ヒドロキシ-L-Orn-]-3β-ヒドロキシ-L-Pro-[(4R,5S)-N2-[(10R,12S)-10,12-ジメチルテトラデカノイル]-4-ヒドロキシ-5-(2-アミノエチルアミノ)-L-Orn*-]]
  • カスポフンギン
  • シクロ[L-Thr-L-t4Hyp-[(3S,4S)-3,4-ジヒドロキシ-4-(4-ヒドロキシフェニル)-L-Abu-]-[(3R)-3-ヒドロキシ-L-Orn-]-[(3S)-3-ヒドロキシ-L-Pro-]-[(4R,5S)-5-[(2-アミノエチル)アミノ]-4-ヒドロキシ-N2-[(10R,12S)-10,12-ジメチル-1-オキソテトラデシル]-L-Orn*-]]
  • (10R,12S)-N-[(3S,6S,9S,11R,15S,18S,20R,21S,24S,25S)-3-[(1R)-3-アミノ-1-ヒドロキシプロピル]-21-[(2-アミノエチル)アミノ]-6-[(1S,2S)-1,2-ジヒドロキシ-2-(4-ヒドロキシフェニル)エチル]-11,20,25-トリヒドロキシ-15-[(1R)-1-ヒドロキシエチル]-2,5,8,14,17,23-ヘキサオキソ-1,4,7,13,16,22-ヘキサアザトリシクロ[22.3.0.09,13]ヘプタコサン-18-イル]-10,12-ジメチルテトラデカンアミド
  • キャスポファンギン
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