5.32280

Myeloperoxidase Inhibitor III, HX1

• 別名: Myeloperoxidase Inhibitor III, HX1, MPO Inhibitor III, HX1
• 実験式（ヒル表記法）: C₁₄H₁₀F₆N₄O₃
• CAS番号: 1520083-61-7
• 分子量: 396.24
• UNSPSCコード: 12352200

特性

• アッセイ: ≥98% (HPLC)
• 品質水準: 100
• 形状: powder
• メーカー／製品名: Calbiochem^®
• 保管条件: OK to freeze; protect from light
• 色: white
• 溶解性: DMSO: 50 mg/mL
• 保管温度: 2-8°C

詳細

詳細

A cell-permeable, trifluoromethyl substituted aromatic hydroxamate compound that acts as a highly potent, selective, mixed type, reversible inhibitor of the chlorination activity of myeloperoxidase (MPO; IC₅₀ = 5 nM). Tightly binds within the active site cavity above the heme and blocks the substrate channel. Displays over 300-fold greater selectivity for MPO when tested against a panel of redox enzymes, including lactoperoxidase (IC₅₀ = 6.3 µM) and thyroid peroxidase (IC₅₀ = 1.59 µM). Blocks the production of hypochlorous acid by human neutrophils (IC₅₀ = 50 nM) and inhibits the formation of NADH bromohydrin (IC₅₀ = 70 nM with 50 µM H₂O₂ and 10 mM NaBr).

A cell-permeable, trifluoromethyl substituted aromatic hydroxamate compound that acts as a highly potent, selective, mixed type, reversible inhibitor of the chlorination activity of myeloperoxidase (MPO; IC₅₀ = 5 nM). Tightly binds within the active site cavity above the heme and blocks the substrate channel. Displays over 300-fold greater selectivity for MPO when tested against a panel of redox enzymes, including lactoperoxidase (IC₅₀ = 6.3 µM) and thyroid peroxidase (IC₅₀ = 1.59 µM). Blocks the production of hypochlorous acid by human neutrophils (IC₅₀ = 50 nM) and inhibits the formation of NADH bromohydrin (IC₅₀ = 70 nM with 50 µM H₂O₂ and 10 mM NaBr).

Please note that the molecular weight for this compound is batch-specific due to variable water content.

生物化学的／生理学的作用

Cell permeable: yes

Primary Target
MPO

警告

Toxicity: Standard Handling (A)

再構成

Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.

その他情報

Forbes, L. V., et al. 2013. J. Bio. Chem.288, 36636.

法的情報

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany

安全性情報

• 保管分類コード: 11 - Combustible Solids
• WGK: WGK 3
• 引火点(°F): Not applicable
• 引火点(℃): Not applicable