525145

sPLA₂-IIA Inhibitor I

The sPLA₂-IIA Inhibitor I controls the biological activity of sPLA₂-IIA. This small molecule/inhibitor is primarily used for Cell Signaling applications.

• Synonyme(s) : sPLA₂-IIA Inhibitor I, c(2NapA)LS(2NapA)R, TFA
• Formule empirique (notation de Hill): C₄₁H₅₀N₈O₆ · xC₂HF₃O₂
• Poids moléculaire : 750.89 (free base basis)
• Code UNSPSC : 41106300
• Nomenclature NACRES : NA.77

Propriétés

• Niveau de qualité: 100
• Pureté: ≥95% (HPLC)
• Forme: lyophilized solid
• Fabricant/nom de marque: Calbiochem^®
• Conditions de stockage: OK to freeze; desiccated (hygroscopic)
• Couleur: white
• Solubilité: DMSO: 5 mg/mL
• Conditions d'expédition: ambient
• Température de stockage: −20°C

Description

Description générale

A highly hydrophobic cyclic pentapeptide that selectively binds and acts as a potent inhibitor of human type IIA secreted phospholipase A₂ (sPLA₂-IIA) (IC₅₀ = 12.8 µM). Reported to effectively block sPLA₂-IIA-induced PGE₂ production at 100 nM in human rheumatoid synoviocytes and is non-toxic at doses up to 10 µM. Does not have any significant effect on the activities of porcine sPLA₂-IB, Naja naja sPLA₂-IB, or Crotalus durissus sPLA₂-IIA at 10 µM.

A highly hydrophobic cyclic pentapeptide that selectively binds and acts as a potent inhibitor of sPLA₂-IIA (human type IIA secreted phospholipase A₂; IC₅₀ = 12.8 μM). Shown to effectively block sPLA₂-IIA-induced PGE₂ production at 100 nM in human rheumatoid synoviocytes and is non-toxic at doses up to 10 μM. Does not have any significant effect on the activities of porcine sPLA₂-IB, Naja naja sPLA₂-IB, or Crotalus durissus sPLA₂-IIA even at 10 μM concentration.

Actions biochimiques/physiologiques

Cell permeable: no

Primary Target
sPLA2-IIA (human type IIA secreted phospholipase A2

Product does not compete with ATP.

Reversible: no

Target IC₅₀: 12.8 µM against sPLA2-IIA (human type IIA secreted phospholipase A2

Conditionnement

Packaged under inert gas

Avertissement

Toxicity: Standard Handling (A)

Séquence

cyclic(2-NaphthylAla-Leu-Ser-2-NaphthylAla-Arg)•TFA

Autres remarques

Church, W.B., et al. 2001. J. Biol. Chem.276, 33156.

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 1
• Point d'éclair (°F): Not applicable
• Point d'éclair (°C): Not applicable