A peptide antagonist of PAR4
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tcY-NH2 (trifluoroacetate salt)

Item No. 36758

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
(S)-N-(2-(((S)-6-amino-1-(((S)-1-amino-1-oxo-3-phenylpropan-2-yl)amino)-1-oxohexan-2-yl)amino)-2-oxoethyl)-1-(cinnamoyl-L-tyrosyl)pyrrolidine-2-carboxamide, trifluoroacetate salt
Synonyms
  • tc-YPGKF-NH2
  • trans-cinnamoyl-YPGKF-amide
  • trans-cinnamoyl-YPGKF-NH2
Molecular Formula
C40H49N7O7 • XCF3COOH
Formula Weight
739.9
Purity
≥98%
Formulation (Request formulation change)
A solid
Solubility(Learn about Variance in Solubility)
DMF: 12 mg/mlDMSO: 10 mg/mlEthanol: 33 mg/mlPBS (pH 7.2): 1 mg/ml
λmax
282 nm
SMILES
NC([C@H](CC1=CC=CC=C1)NC([C@H](CCCCN)NC(CNC([C@H]2N(C([C@@H](NC(/C=C/C3=CC=CC=C3)=O)CC4=CC=C(O)C=C4)=O)CCC2)=O)=O)=O)=O.OC(C(F)(F)F)=O
InChi Code
InChI=1S/C40H49N7O7.C2HF3O2/c41-22-8-7-14-31(38(52)46-32(37(42)51)24-28-12-5-2-6-13-28)44-36(50)26-43-39(53)34-15-9-23-47(34)40(54)33(25-29-16-19-30(48)20-17-29)45-35(49)21-18-27-10-3-1-4-11-27;3-2(4,5)1(6)7/h1-6,10-13,16-21,31-34,48H,7-9,14-15,22-26,41H2,(H2,42,51)(H,43,53)(H,44,50)(H,45,49)(H,46,52);(H,6,7)/b21-18+;/t31-,32-,33-,34-;/m0./s1
InChi Key
WQJKBSZTPQERHW-USBDLMLUSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    500 µg

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    1 mg

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    5 mg

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    10 mg

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    Product Description

    tcY-NH2 is a synthetic peptide antagonist of proteinase-activated receptor 4 (PAR4) that corresponds to amino acids 1-6 of the amino terminal tethered ligand sequence of mouse PAR4.1 It inhibits platelet aggregation induced by the PAR4 agonist AYPGKF-NH2 (Item No. 24258) in washed isolated rat platelets (IC50 = 95-190 µM), as well as induces relaxation of isolated rat aortic rings precontracted with phenylephrine and contraction of isolated rat gastric longitudinal muscle strips (EC50s = 64 and 1 µM, respectively). tcY-NH2 (400 µM) inhibits thrombin-induced migration of primary hepatocellular carcinoma (HCC) cells.2 It reduces myocardial infarct size as a percentage of the area at risk ex vivo in a isolated rat heart model of ischemia-reperfusion injury.3

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Hollenberg, M.D., Saifeddine, M., Sandhu, S., et al. Proteinase-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).

    2. Kaufmann, R., Rahn, S., Pollrich, K., et al. Thrombin-mediated hepatocellular carcinoma cell migration: Cooperative action via proteinase-activated receptors 1 and 4. J. Cell. Physiol. 211(3), 699-707 (2007).

    3. Strande, J.L., Hsu, A., Su, J., et al. Inhibiting protease-activated receptor 4 limits myocardial ischemia/reperfusion injury in rat hearts by unmasking adenosine signaling. J. Pharmacol. Exp. Ther. 324(3), 1045-1054 (2008).