5.32280

Myeloperoxidase Inhibitor III, HX1

• Sinônimo(s): Myeloperoxidase Inhibitor III, HX1, MPO Inhibitor III, HX1
• Fórmula empírica (Notação de Hill): C₁₄H₁₀F₆N₄O₃
• Número CAS: 1520083-61-7
• Peso molecular: 396.24
• Código UNSPSC: 12352200

Propriedades

• Ensaio: ≥98% (HPLC)
• Nível de qualidade: 100
• Formulário: powder
• fabricante/nome comercial: Calbiochem^®
• condição de armazenamento: OK to freeze; protect from light
• cor: white
• solubilidade: DMSO: 50 mg/mL
• temperatura de armazenamento: 2-8°C

Descrição

Descrição geral

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.

Ações bioquímicas/fisiológicas

Cell permeable: yes

Primary Target
MPO

Advertência

Toxicity: Standard Handling (A)

Reconstituição

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

Outras notas

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

Informações legais

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

Informações de segurança

• Código de classe de armazenamento: 11 - Combustible Solids
• Classe de risco de água (WGK): WGK 3
• Ponto de fulgor (°F): Not applicable
• Ponto de fulgor (°C): Not applicable