5.32280

Myeloperoxidase Inhibitor III, HX1

• Synonyme(s) : Myeloperoxidase Inhibitor III, HX1, MPO Inhibitor III, HX1
• Formule empirique (notation de Hill): C₁₄H₁₀F₆N₄O₃
• Numéro CAS: 1520083-61-7
• Poids moléculaire : 396.24
• Code UNSPSC : 12352200

Propriétés

• Pureté: ≥98% (HPLC)
• Niveau de qualité: 100
• Forme: powder
• Fabricant/nom de marque: Calbiochem^®
• Conditions de stockage: OK to freeze; protect from light
• Couleur: white
• Solubilité: DMSO: 50 mg/mL
• Température de stockage: 2-8°C

Description

Description générale

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.

Actions biochimiques/physiologiques

Cell permeable: yes

Primary Target
MPO

Avertissement

Toxicity: Standard Handling (A)

Reconstitution

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

Autres remarques

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

Informations légales

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

Informations sur la sécurité

• Code de la classe de stockage: 11 - Combustible Solids
• Classe de danger pour l'eau (WGK): WGK 3
• Point d'éclair (°F): Not applicable
• Point d'éclair (°C): Not applicable