Parstatin (human)

CAS No. 1065755-99-8

Parstatin (human)( —— )

Catalog No. M30597 CAS No. 1065755-99-8

Cell-permeable peptide cleaved from protease-activated receptor 1 (PAR1) upon receptor activation. Attenuates endothelial cell migration and proliferation (IC50 ~ 3 μM), and induces cell cycle arrest. Promotes activation of caspase-3 and exhibits pro-apoptotic activity in vitro. Inhibits angiogenesis and exhibits cardioprotective activity in vivo.

Purity : >98% (HPLC)

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Biological Information

  • Product Name
    Parstatin (human)
  • Note
    Research use only, not for human use.
  • Brief Description
    Cell-permeable peptide cleaved from protease-activated receptor 1 (PAR1) upon receptor activation. Attenuates endothelial cell migration and proliferation (IC50 ~ 3 μM), and induces cell cycle arrest. Promotes activation of caspase-3 and exhibits pro-apoptotic activity in vitro. Inhibits angiogenesis and exhibits cardioprotective activity in vivo.
  • Description
    Cell-permeable peptide cleaved from protease-activated receptor 1 (PAR1) upon receptor activation. Attenuates endothelial cell migration and proliferation (IC50 ~ 3 μM), and induces cell cycle arrest. Promotes activation of caspase-3 and exhibits pro-apoptotic activity in vitro. Inhibits angiogenesis and exhibits cardioprotective activity in vivo.
  • In Vitro
    Parstatin (0-10 μM) increases recovery of LVDP in a concentration-dependent manner. The optimal concentration was 1 μM which produced a 23% recovery of LVDP.
  • In Vivo
    Parstatin (single dose, 1-25 μg/kg, iv) administered prior to ischaemia confers immediate cardioprotection by recruiting the Gi-protein activation pathway including p38 MAPK, ERK1/2, NOS, and KATP channels. Parstatin exerts effects on both the cardiomyocytes and the coronary circulation to induce cardioprotection. This suggests a potential therapeutic role of parstatin in the treatment of cardiac injury resulting from ischaemia and reperfusion. Animal Model:Male Sprague–Dawley rats at 8 weeks of age (250-300 g).Dosage:1-25 μg/kg.Administration:IV injected 15 min prior to ischaemia.Result:A significant decrease in infarct size was detected with the 5-15 μg/kg doses with 10 μg/kg as the optimal dose. These hearts had an infarct size of 46 ± 3% of the area at risk, which is a 26% reduction in infarct size compared with the control.
  • Synonyms
    ——
  • Pathway
    GPCR/G Protein
  • Target
    PAR
  • Recptor
    ——
  • Research Area
    ——
  • Indication
    ——

Chemical Information

  • CAS Number
    1065755-99-8
  • Formula Weight
    4467.29
  • Molecular Formula
    C191H330N64O53S3
  • Purity
    >98% (HPLC)
  • Solubility
    water:1 mg/mL
  • SMILES
    [H]N[C@@H](CCSC)C(=O)NCC(=O)N1CCC[C@H]1C(=O)N[C@@H](CCCNC(N)=N)C(=O)N[C@@H](CCCNC(N)=N)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](C(C)C)C(=O)N[C@@H](C)C(=O)N[C@@H](C)C(=O)N[C@@H](CS)C(=O)N[C@@H](CC1=CC=CC=C1)C(=O)N[C@@H](CO)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CS)C(=O)NCC(=O)N1CCC[C@H]1C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CO)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCNC(N)=N)C(=O)N[C@@H]([C@@H](C)O)C(=O)N[C@@H](CCCNC(N)=N)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCNC(N)=N)C(=O)N[C@@H](CCCNC(N)=N)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCC(O)=O)C(=O)N[C@@H](CO)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](C)C(=O)N[C@@H]([C@@H](C)O)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](C)C(=O)N[C@@H]([C@@H](C)O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(O)=O)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCCNC(N)=N)C(O)=O
  • Chemical Name
    ——

Shipping & Storage Information

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

Reference

1. Zania et al (2009) Parstatin, the cleaved peptide on proteinase-activated receptor 1 activation, is a potent inhibitor of activation. J.Pharmacol.Exp.Ther. 328 378 PMID:
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