A peptide agonist of PAR4
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(Ala1)-PAR4 (1-6) amide (mouse) (trifluoroacetate salt)

Item No. 24258

Technical Information
Formal Name
L-alanyl-L-tyrosyl-L-prolylglycyl-L-lysyl-L-phenylalaninamide, trifluoroacetate salt
Synonyms
  • AY-NH2
  • AYPGKF-NH2
  • H-Ala-Tyr-Pro-Gly-Lys-Phe-NH2
  • PAR4-AP
  • Proteinase-Activated Receptor 4 Activating Peptide
Molecular Formula
C34H48N8O7 • XCF3COOH
Formula Weight
Purity
≥95%
A lyophilized powder
Water: 1 mg/ml
SMILES
NC([C@@H](NC([C@H](CCCCN)NC(CNC([C@H]1N(C([C@H](CC2=CC=C(O)C=C2)NC([C@H](C)N)=O)=O)CCC1)=O)=O)=O)CC3=CC=CC=C3)=O.FC(F)(C(O)=O)F
InChi Code
InChI=1S/C34H48N8O7.C2HF3O2/c1-21(36)31(46)41-27(19-23-12-14-24(43)15-13-23)34(49)42-17-7-11-28(42)33(48)38-20-29(44)39-25(10-5-6-16-35)32(47)40-26(30(37)45)18-22-8-3-2-4-9-22;3-2(4,5)1(6)7/h2-4,8-9,12-15,21,25-28,43H,5-7,10-11,16-20,35-36H2,1H3,(H2,37,45)(H,38,48)(H,39,44)(H,40,47)(H,41,46);(H,6,7)/t21-,25-,26-,27-,28-;/m0./s1
InChi Key
BGPJLFVICWHITH-HKJXYENISA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    Product Description

    (Ala1)-PAR4 (1-6) amide (mouse) is a peptide agonist of proteinase-activated receptor 4 (PAR4) that induces aggregation of rat and human platelets in vitro (EC50s = 15 and 60 μM, respectively).1,2 It reduces expression of glycoprotein (GP) Ib, and increases expression of GPIIb/IIIa on the surface of human platelets.2 (Ala1)-PAR4 (1-6) amide (mouse) induces relaxation of isolated rat aortic rings and contraction of rat gastric longitudinal muscle strips (EC50s = 11 and 110 μM, respectively) as well as inhibits calcium mobilization evoked by capsaicin (Item No. 92350) in rat sensory neurons.3,4 In vivo, (Ala1)-PAR4 (1-6) amide (mouse) (1-100 µg) increases latency to paw withdrawal and the nociceptive threshold in response to thermal and mechanical stimuli.4 (Ala1)-PAR4 (1-6) amide (mouse) (200 µg) also increases paw thickness in a rat paw edema assay.

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Hollenberg, M.D., and Saifeddine, M. Proteinase-activated receptor 4 (PAR4): Activation and inhibition of rat platelet aggregation by PAR4-derived peptides. Can. J. Physiol. Pharmacol. 79(5), 439-442 (2001).

    2. Chung, A.W., Jurasz, P., Hollenberg, M.D., et alMechanisms of action of proteinase-activated receptor agonists on human platelets. Br. J. Pharmacol. 135(5), 1123-1132 (2002).

    3. Hollenberg, M.D., Saifeddine, M., Sandhu, S., et alProteinase-activated receptor-4: Evaluation of tethered ligand-derived peptides as probes for receptor function and as inflammatory agonists in vivo. Br. J. Pharmacol. 143(4), 443-454 (2004).

    4. Asfaha, S., Cenac, N., Houle, S., et alProtease-activated receptor-4: A novel mechanism of inflammatory pain modulation. Br. J. Pharmacol. 150(2), 176-185 (2007).