5.30538

cPLA2α Inhibitor II, Pyrrophenone

• Synonyme(s) : cPLA2α Inhibitor II, Pyrrophenone, Phospholipase A2α Inhibitor
• Formule empirique (notation de Hill): C₄₉H₃₇F₂N₃O₅S₂
• Numéro CAS: 341973-06-6
• Poids moléculaire : 849.96
• Code UNSPSC : 12352200

Propriétés

• Pureté: ≥98% (HPLC)
• Niveau de qualité: 100
• Forme: powder
• Puissance: 4.2 nM IC₅₀
• Fabricant/nom de marque: Calbiochem^®
• Conditions de stockage: OK to freeze; protect from light
• Couleur: off-white
• Solubilité: DMSO: 100 mg/mL
• Température de stockage: −20°C

Description

Description générale

A cell-permeable, non-toxic, pyrolidine derivative that acts as a highly potent, and reversible inhibitor of cytosolic phospholipase A2a (cPLA2a; IC₅₀ = 4.2 nM). Does not inhibit the activities of PLA IB and IIA groups even at higher concentrations (~250 µM). Unlike AACOCF3 (Cat. No. 100109), its action is shown to be rapid and does not require a pre-incubation period. Diminishes the release of arachidonic acid (IC₅₀ = 24 nM), prostaglandin E2 (PGE2; IC₅₀ = 25 nM) and leukotriene C4 (IC₅₀ = 14 nM) in A23187 stimulated THP-1 cells. Its effects on production of PGE2 and thromboxane B2 are comparable to those of indomethacin. Also shown to inhibit the lysophospholipase and esterase activity of cPLA2&alpha.

A cell-permeable, non-toxic, pyrolidine derivative that acts as a highly potent, and reversible inhibitor of cytosolic phospholipase A2a (cPLA2a; IC₅₀ = 4.2 nM). Does not inhibit the activities of PLA IB and IIA groups even at higher concentrations (~250 µM). Unlike AACOCF3 (Cat. No. 100109), its action is shown to be rapid and does not require a pre-incubation period. Diminishes the release of arachidonic acid (IC₅₀ = 24 nM), prostaglandin E2 (PGE2; IC₅₀ = 25 nM) and leukotriene C4 (IC₅₀ = 14 nM) in A23187 stimulated THP-1 cells. Its effects on production of PGE2 and thromboxane B2 are comparable to those of indomethacin. Also shown to inhibit the lysophospholipase and esterase activity of cPLA2&alpha.

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
PLA2a

Conditionnement

Packaged under inert gas

Avertissement

Toxicity: Standard Handling (A)

Autres remarques

Ono, T., et al. 2002. Biochem. J.363, 727.
Seno, K., et al. 2001. Bioorg. Med. Chem. Lett.11, 587.

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