Formulation: A solid
Formal Name: L-seryl-L-phenylalanyl-L-phenylalanyl-L-leucyl-L-arginyl-L-asparagine, trifluoroacetate salt
Purity: ≥95%
Formula Markup: C37H54N10O9 • XCF3COOH
Formula Weight: 782,9
Shelf life (days): 1460
Notes: PAR1 (1-6) is a hexapeptide that corresponds to amino acid residues 1-6 of the amino terminal tethered ligand sequence of mouse and rat proteinase-activated receptor 1 (PAR1), residues 42-47 of the full-length mouse sequence, and residues 46-51 of the full-length rat sequence.{46158,46159} PAR1 is a high-affinity thrombin receptor that induces platelet activation and deposition into thrombi as well as smooth muscle mitogenesis.{46160} Unlike thrombin, PAR1 (1-6) acts as an agonist of PAR1 in smooth muscle cells but is inactive in rodent platelets.{46161} It increases mitogenesis and the expression of the IGF-1 receptor (IGF-1R) by 47% in vascular smooth muscle cells (VSMCs), an effect that is inhibited by the thrombin inhibitor hirudin and by the protein tyrosine kinase inhibitor genistein (Item No. 10005167).{46159} PAR1 (1-6) increases histamine and β-hexosaminidase release from rat peritoneal mast cells in a concentration-dependent manner, with the maximum release at a concentration of 50 µM.{46158} It also mimics the effect of thrombin, increasing swelling-activated efflux of [3H]glutamate induced by hypoosmotic medium in astrocytes in vitro when used at concentrations ranging from 5 to 10 µM.{46162}
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