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.

• Sinónimos: sPLA₂-IIA Inhibitor I, c(2NapA)LS(2NapA)R, TFA
• Fórmula empírica (notación de Hill): C₄₁H₅₀N₈O₆ · xC₂HF₃O₂
• Peso molecular: 750.89 (free base basis)
• UNSPSC Code: 41106300
• NACRES: NA.77

Propiedades

• Quality Level: 100
• assay: ≥95% (HPLC)
• form: lyophilized solid
• manufacturer/tradename: Calbiochem^®
• storage condition: OK to freeze; desiccated (hygroscopic)
• color: white
• solubility: DMSO: 5 mg/mL
• shipped in: ambient
• storage temp.: −20°C

Descripción

General description

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.

Biochem/physiol Actions

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

Packaging

Packaged under inert gas

Warning

Toxicity: Standard Handling (A)

Sequence

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

Other Notes

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

Legal Information

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

Información de seguridad

• Storage Class: 11 - Combustible Solids
• wgk_germany: WGK 1
• flash_point_f: Not applicable
• flash_point_c: Not applicable