P2pal-18S is a cell-penetrating proteinase-activated receptor-2 (PAR2) antagonist, designed from a structural model of the PAR2 dimer. P2pal-18S is highly selective for PAR2 and has no antagonist activity at the closely related PAR1, PAR4, or CXCR1/2 IL-8 receptors in neutrophil chemotaxis assays. In vitro, P2pal-18S completely suppresses trypsin and mast cell tryptase signaling through PAR2 in neutrophils and colon cancer cells, and in vivo, it is highly efficacious in blocking PAR2-dependent inflammatory responses, preventing the development of neuroinflammatory disease in murine models of multiple sclerosis and experimental autoimmune encephalomyelitis (EAE).
Molekulargewicht:
2302.77
Reinheit:
>95% BPLC
Formulierung:
Freeze dried solid
Sequenz:
Palmitoyl-RSSAMDENSEKKRKSAIK-NH2
Formel:
C99H180N30O30S
Target-Kategorie:
Protease activated receptors
Anwendungsbeschreibung:
ProductType: Cell penetrating peptides
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