A PAR2 agonist
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SLIGRL-NH2 (trifluoroacetate salt)

Item No. 16723

Technical Information
Formal Name
L-seryl-L-leucyl-L-isoleucylglycyl-L-arginyl-L-Leucinamide, trifluoroacetate salt
Molecular Formula
C29H56N10O7 • XCF3COOH
Formula Weight
Purity
≥98%
A crystalline solid
DMF: 20 mg/mlDMSO: 20 mg/mlEthanol: 5 mg/mlPBS (pH 7.2): 10 mg/ml
SMILES
NC(NCCC[C@H](NC(CNC([C@H]([C@H](CC)C)NC([C@@H](NC([C@H](CO)N)=O)CC(C)C)=O)=O)=O)C(N[C@H](C(N)=O)CC(C)C)=O)=N.FC(F)(C(O)=O)F
InChi Code
InChI=1S/C29H56N10O7.C2HF3O2/c1-7-17(6)23(39-27(45)21(12-16(4)5)38-25(43)18(30)14-40)28(46)35-13-22(41)36-19(9-8-10-34-29(32)33)26(44)37-20(24(31)42)11-15(2)3;3-2(4,5)1(6)7/h15-21,23,40H,7-14,30H2,1-6H3,(H2,31,42)(H,35,46)(H,36,41)(H,37,44)(H,38,43)(H,39,45)(H4,32,33,34);(H,6,7)/t17-,18-,19-,20-,21-,23-;/m0./s1
InChi Key
LVEFPJRPZFTZBQ-DBYSMBDASA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    Product Description

    SLIGRL-NH2 is a recombinant peptide that activates PAR2 (EC50 = ~5 µM), without requiring receptor cleavage.1,2 This peptide does not activate PAR1. Through its effects on PAR2, SLIGRL-NH2 stimulates gastric and intestinal smooth muscle contraction and induces thermal hyperalgesia in mice.3,4 SLIGRL-NH2 is used to explore signaling through PAR2 in cells and in animals.5,6

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Nystedt, S., Emilsson, K., Wahlestedt, C., et alMolecular cloning of a potential proteinase activated receptor. Proc. Natl. Acad. Sci. USA 97(20), 9208-9212 (1994).

    2. Nystedt, S., Larsson, A.K., Aberg, H., et alThe mouse proteinase-activated receptor-2 cDNA and gene. Molecular cloning and functional expression. The Journal of Biological Chemisty 270(11), 5950-5955 (1995).

    3. Kawabata, A., Kuroda, R., Nagata, N., et alIn vivo evidence that protease-activated receptors 1 and 2 modulate gastrointestinal transit in the mouse. Br. J. Pharmacol. 133(8), 1213-1218 (2001).

    4. Liu, Q., Weng, H.J., Patel, K.N., et alThe distinct roles of two GPCRs, MrgprC11 and PAR2, in itch and hyperalgesia. Sci. Signal. 4(181), 1-6 (2011).

    5. Sriwai, W., Mahavadi, S., Al-Shboul, O., et alDistinctive G protein-dependent signaling by protease-activated receptor 2 (PAR2) in smooth muscle: Feedback inhibition of RhoA by cAMP-independent PKA. PLoS One 8(6), 1-12 (2013).

    6. Elmariah, S.B., Reddy, V.B., and Lerner, E.A. Cathepsin S signals via PAR2 and generates a novel tethered ligand receptor agonist. PLoS One 9(6), 1-9 (2014).