A peptide agonist of PAR2
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PAR2 (1-6) amide (human) (trifluoroacetate salt)

Item No. 35204

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
L-seryl-L-leucyl-L-isoleucylglycyl-L-lysyl-L-valinamide, trifluoroacetate salt
CAS Number
2379569-17-0
Synonyms
  • SLIGKV-NH2
Molecular Formula
C28H54N8O7 • XCF3COOH
Formula Weight
614.8
Purity
≥95%
Formulation (Request formulation change)
A solid
Solubility(Learn about Variance in Solubility)
DMF: 30 mg/mlDMSO: 15 mg/mlEthanol: 5 mg/mlPBS (pH 7.2): 10 mg/ml
SMILES
OC[C@H](N)C(N[C@@H](CC(C)C)C(N[C@@H]([C@@H](C)CC)C(NCC(N[C@@H](CCCCN)C(N[C@H](C(N)=O)C(C)C)=O)=O)=O)=O)=O.FC(F)(C(O)=O)F
InChi Code
InChI=1S/C28H54N8O7.C2HF3O2/c1-7-17(6)23(36-27(42)20(12-15(2)3)34-25(40)18(30)14-37)28(43)32-13-21(38)33-19(10-8-9-11-29)26(41)35-22(16(4)5)24(31)39;3-2(4,5)1(6)7/h15-20,22-23,37H,7-14,29-30H2,1-6H3,(H2,31,39)(H,32,43)(H,33,38)(H,34,40)(H,35,41)(H,36,42);(H,6,7)/t17-,18-,19-,20-,22-,23-;/m0./s1
InChi Key
HZTZARICKSBEFA-HZIHITNPSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    5 mg

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    25 mg

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    Product Description

    PAR2 (1-6) amide is a synthetic peptide agonist of proteinase-activated receptor 2 (PAR2) that corresponds to residues 1-6 of the amino terminal tethered ligand sequence of human PAR2 and residues 37-42 of the full-length sequence.1 It binds to NCTC 2544 cells expressing human PAR2 (Ki = 9.64 µM in a radioligand binding assay) and induces calcium mobilization in the same cells (EC50 = 0.075 µM).2 PAR2 (1-6) amide (100 µM) reduces colony formation of A549 lung cancer cells.1 It induces superoxide production and degranulation in isolated human eosinophils when used at a concentration of 500 µM.3 PAR2 (1-6) amide (5 µmol/kg) induces tear secretion in rats when used in combination with amastatin (Item No. 16719).4

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Bohm, S.K., Kong, W., Bromme, D., et al. Molecular cloning, expression and potential functions of the human proteinase-activated receptor-2. Biochem. J. 314(Pt 3), 1009-1016 (1996).

    2. Kanke, T., Ishiwata, H., Kabeya, M., et al. Binding of a highly potent protease-activated receptor-2 (PAR2) activating peptide, [3H]2-furoyl-LIGRL-NH2, to human PAR2. Br. J. Pharmacol. 145(2), 255-263 (2005).

    3. Miike, S., McWilliam, A.S., and Kita, H. Trypsin induces activation and inflammatory mediator release from human eosinophils through protease-activated receptor-2. J. Immunol. 167(11), 6615-6622 (2001).

    4. Nishikawa, H., Kawai, K., Tanaka, M., et al. Protease-activated receptor-2 (PAR-2)-related peptides induce tear secretion in rats: Involvement of PAR-2 and non-PAR-2 mechanisms. J. Pharmacol. Exp. Ther. 312(2), 324-331 (2005).