シベレスタット ナトリウム塩 水和物

シベレスタット ナトリウム塩 水和物 価格

シベレスタット ナトリウム塩 水和物 化学特性,用途語,生産方法

• 効能

  炎症性疾患治療薬, エラスターゼ阻害薬

• 使用

  Sivelestat is an inhibitor of neutrophil elastase that prevents neutrophil extracellular trap formation and rescues mice from endotoxic shock. The inhibition of neutropil elastase by Sivelestat is a promising therapeutic strategy to inhibit glial scar and promote functional recovery by upregulating angiopoietin-1 after spinal cord injury.

• 一般的な説明

  A cell-permeable, potent, substrate-competitive, and highly specific inhibitor of neutrophil elastase (IC₅₀ = 19-49 nM using rat, rabbit, hamster, human, and mouse leukocyte elastase). Displays about 100-fold greater selectivity over pancreatic elastase (IC₅₀ = 5.6 μM) and is inactive against trypsin, thrombin, plasmin, kallikrein, chymotrypsin, and cathepsin G even at concentrations as high as 100 μM. Effectively suppresses human neutrophil elastase-induced lung hemorrhage and skin capillary permeability in vivo. Also reported to inhibit mast cell Stat6-protease.

• Biochem/physiol Actions

  Sivelestat is a competitive human neutrophil elastase (HNE) inhibitor (IC50 = 44 nM, Ki = 0.2 μM). It also inhibits leukocyte elastase obtained from rabbit, rat, hamster and mouse (IC50 = 19 to 49 nM). However, it does not inhibit trypsin, thrombin, plasmin, plasma kallikrein, pancreas kallikrein, chymotrypsin and cathepsin G even at 100 μM. In in-vivo studies, it suppressed lung hemorrhage in hamster (ID50 = 82 μg/kg) by intratracheal administration and increase of skin capillary permeability in guinea pig (ID50 = 9.6 mg/kg) by intravenous administration, both of which were induced by human neutrophil elastase.

シベレスタット ナトリウム塩 水和物 生産企業

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シベレスタット ナトリウム塩 水和物 スペクトルデータ(¹HNMR)

127373-66-4, シベレスタット ナトリウム塩 水和物 キーワード