tcY-NH2

CAS No. 327177-34-4

tcY-NH2( —— )

Catalog No. M30778 CAS No. 327177-34-4

Selective PAR4 antagonist peptide. Inhibits endostatin release and platelet aggregation induced by thrombin.

Purity : >98% (HPLC)

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Biological Information

  • Product Name
    tcY-NH2
  • Note
    Research use only, not for human use.
  • Brief Description
    Selective PAR4 antagonist peptide. Inhibits endostatin release and platelet aggregation induced by thrombin.
  • Description
    Selective PAR4 antagonist peptide. Inhibits endostatin release and platelet aggregation induced by thrombin.
  • In Vitro
    tcY-NH2 (0-500 μM) inhibits AYPGKF-NH2 (10 μM)-induced platelet (obtained from male albino Sprague–Dawley rats) aggregation, with an IC50 value of 95 μM.tcY-NH2 potently activates aorta relaxation (RA) and gastric (LM) contraction, with IC50 values of 64 μM (RA) and 1 μM (LM).tcY-NH2 (Tc-YPGKF-NH2, 400 μM, 5 min) prevents endostatin release and platelet aggregation induced by thrombin or by AY-NH2.tcY-NH2 (5 μM, 15 min) decreases infarct size (IS) by 51%, and increases recovery of ventricular function by 26% in an isolated heart model.
  • In Vivo
    tcY-NH2 (tail vein injection, 0.6 mg/kg for a single dose) alleviates liver injury in Brain death (BD) rat model, indicated by lower serum ALT/AST levels and better histomorphology.tcY-NH2 (intraperitoneal injection, 0.6 mg/kg for a single dose) increases posttraumatic activation of CD4+ Tregs within the draining lymph nodes in burn injury mice model .tcY-NH2 (intrapleural injection, 40 ng/kg for a single dose) inhibits neutrophil recruitment in experimental inflammation in mice. Animal Model:Brain death (BD) rat model Dosage:0.6 mg/kg for a single doseAdministration:Tail vein injection for a single dose Result:Reduced blood platelet activation and hepatic platelet accumulation.Attenuated the inflammatory response and apoptosis in the livers.Inhibited the activation of NF-κB and MAPK pathways induced by Brain death (BD).Animal Model:Burn injury model of C57BL/6 N mice Dosage:0.6 mg/kg for a single dose Administration:Intraperitoneal injection Result:Increased expression and phosphorylation of PKC-θ in the presence of platelets, without affecting early posttraumatic hemostasis.Animal Model:BALB/c mice Dosage:40 ng/kg for a single dose Administration:Intrapleural injection Result:Abolished the number of rolling and adhering neutrophils on the vessel wall.Inhibited CXCL8- and Cg-induced neutrophil migration into the pleural cavity of mice.
  • Synonyms
    ——
  • Pathway
    GPCR/G Protein
  • Target
    PAR
  • Recptor
    ——
  • Research Area
    ——
  • Indication
    ——

Chemical Information

  • CAS Number
    327177-34-4
  • Formula Weight
    739.87
  • Molecular Formula
    C40H49N7O7
  • Purity
    >98% (HPLC)
  • Solubility
    water:1 mg/mL
  • SMILES
    NCCCC[C@H](NC(=O)CNC(=O)[C@@H]1CCCN1C(=O)[C@H](CC1=CC=C(O)C=C1)NC(=O)\C=C\C1=CC=CC=C1)C(=O)N[C@@H](CC1=CC=CC=C1)C(N)=O
  • Chemical Name
    ——

Shipping & Storage Information

  • Storage
    (-20℃)
  • Shipping
    With Ice Pack
  • Stability
    ≥ 2 years

Reference

1. Hollenberg et al (2004) Proteinase-activated receptor-4: evaluation of tethered ligand-derived peptides as probes for receptor function and as inflammatory agonists in vivo. Br.J.Pharmacol. 143 443 PMID:
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