PAR1 (1-6) (mouse, rat) (trifluoroacetate salt)

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.1,2 PAR1 is a high-affinity thrombin receptor that induces platelet activation and deposition into thrombi as well as smooth muscle mitogenesis.3 Unlike thrombin, PAR1 (1-6) acts as an agonist of PAR1 in smooth muscle cells but is inactive in rodent platelets.4 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).2 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.1 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.5WARNING This product is not for human or veterinary use.

[1] TAMARA N. DUGINA . Activation of mast cells induced by agonists of proteinase-activated receptors under normal conditions and during acute inflammation in rats[J]. European journal of pharmacology, 2003, 471 2: Pages 141-147. DOI: 10.1016/s0014-2999(03)01752-7
[2] JIE DU. Thrombin Regulates Insulin-Like Growth Factor-1 Receptor Transcription in Vascular Smooth Muscle: Characterization of the Signaling Pathway[J]. Circulation Research: Journal of the American Heart Association, 2001, 37 1: 1044-1052. DOI: 10.1161/hh1001.090840
[3] TEJMINDER S SIDHU J R H Shauna L French. Differential signaling by protease-activated receptors: implications for therapeutic targeting.[J]. International Journal of Molecular Sciences, 2014, 15 4: 6169-6183. DOI: 10.3390/ijms15046169
[4] CLAUDIA K. DERIAN. Species differences in platelet responses to thrombin and SFLLRN. Receptor-mediated calcium mobilization and aggregation, and regulation by protein kinases[J]. Thrombosis research, 1995, 78 6: Pages 505-519. DOI: 10.1016/0049-3848(95)00084-5
[5] GERARDO RAMOS-MANDUJANO. Thrombin potently enhances swelling-sensitive glutamate efflux from cultured astrocytes[J]. Glia, 2007, 55 9: 917-925. DOI: 10.1002/glia.20513