A peptide agonist of PAR1
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PAR1 (1-6) (mouse, rat) (trifluoroacetate salt)

Item No. 27111

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
L-seryl-L-phenylalanyl-L-phenylalanyl-L-leucyl-L-arginyl-L-asparagine, trifluoroacetate salt
Synonyms
  • H-Ser-Phe-Phe-Leu-Arg-Asn
  • PAR1-AP
  • Proteinase-Activated Receptor 1
  • SFFLRN
  • TRAP
  • Thrombin Receptor Activating Peptide
Molecular Formula
C37H54N10O9 • XCF3COOH
Formula Weight
782.9
Purity
≥95%
Formulation (Request formulation change)
A solid
Solubility(Learn about Variance in Solubility)
Water: 1 mg/ml
SMILES
[H]N[C@@H](CO)C(N[C@H](C(N[C@H](C(N[C@@H](CC(C)C)C(N[C@@H](CCCNC(N)=N)C(N[C@@H](CC(N)=O)C(O)=O)=O)=O)=O)CC1=CC=CC=C1)=O)CC2=CC=CC=C2)=O.OC(C(F)(F)F)=O
InChi Code
InChI=1S/C37H54N10O9.C2HF3O2/c1-21(2)16-26(33(52)43-25(14-9-15-42-37(40)41)32(51)47-29(36(55)56)19-30(39)49)45-35(54)28(18-23-12-7-4-8-13-23)46-34(53)27(44-31(50)24(38)20-48)17-22-10-5-3-6-11-22;3-2(4,5)1(6)7/h3-8,10-13,21,24-29,48H,9,14-20,38H2,1-2H3,(H2,39,49)(H,43,52)(H,44,50)(H,45,54)(H,46,53)(H,47,51)(H,55,56)(H4,40,41,42);(H,6,7)/t24-,25-,26-,27-,28-,29-;/m0./s1
InChi Key
NTVASBVJSJIDKA-IGCYJKAMSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    Product Description

    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.5

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Dugina, T.N., Kiseleva, E.V., Glusa, E., et al. Activation of mast cells induced by agonists of proteinase-activated receptors under normal conditions and during acute inflammation in rats. Eur. J. Pharmacol. 471(2), 141-147 (2003).

    2. Du, J., Brink, M., Peng, T., et al. Thrombin regulates insulin-like growth factor-1 receptor transcription in vascular smooth muscle: Characterization of the signaling pathway. Circ. Res. 88(10), 1044-1052 (2001).

    3. Sidhu, T.S., French, S.L., and Hamilton, J.R. Differential signaling by protease-activated receptors: Implications for therapeutic targeting. Int. J. Mol. Sci. 15(4), 6169-6183 (2014).

    4. Derian, C.K., Santulli, R.J., Tomko, K.A., et al. Species differences in platelet responses to thrombin and SFLLRN. receptor-mediated calcium mobilization and aggregation, and regulation by protein kinases. Thromb. Res. 78(6), 505-519 (1995).

    5. Ramos-Mandujano, G., Vázquez-Juárez, E., Hernández-Benítez, R., et al. Thrombin potently enhances swelling-sensitive glutamate efflux from cultured astrocytes. Glia 55(9), 917-925 (2007).