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PA-8

CAS No. 878437-15-1

PA-8( —— )

Catalog No. M35242 CAS No. 878437-15-1

PA-8 is a small molecule receptor antagonist for PACAP Type I (PAC1) that is selective, effective, and orally active. PA-8 inhibits PacAP-induced CREB phosphorylation at PAC1- receptors, but does not inhibit VPAC1- or vpac2 receptors.

Purity : >98% (HPLC)

COA Datasheet HNMR HPLC MSDS Handing Instructions
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Biological Information

  • Product Name
    PA-8
  • Note
    Research use only, not for human use.
  • Brief Description
    PA-8 is a small molecule receptor antagonist for PACAP Type I (PAC1) that is selective, effective, and orally active. PA-8 inhibits PacAP-induced CREB phosphorylation at PAC1- receptors, but does not inhibit VPAC1- or vpac2 receptors.
  • Description
    PA-8 is a potent, selective and orally active PACAP type I (PAC1) receptor antagonist. PA-8 inhibits the phosphorylation of CREB induced by PACAP in PAC1-, but not VPAC1- or VPAC2-receptor. PA-8 also inhibits PACAP-induced cAMP elevation with an IC50 of 2 nM.
  • In Vitro
    ——
  • In Vivo
    Animal Model:Male ddY mice (6 weeks old) injected with PACAP (100 pmol) Dosage:100 pmol/5 μL Administration:Intrathecal injection; once Result:Inhibited PACAP-induced aversive responses and mechanical allodynia in vivo.
  • Synonyms
    ——
  • Pathway
    Others
  • Target
    Other Targets
  • Recptor
    PACAP
  • Research Area
    ——
  • Indication
    ——

Chemical Information

  • CAS Number
    878437-15-1
  • Formula Weight
    342.35
  • Molecular Formula
    C17H18N4O4
  • Purity
    >98% (HPLC)
  • Solubility
    In Vitro:?DMSO : 25 mg/mL (73.02 mM; Ultrasonic (<60°C)
  • SMILES
    COc1cc(ccc1OCC=C)C1CC(=O)Nc2nc(N)[nH]c(=O)c12
  • Chemical Name
    ——

Shipping & Storage Information

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

Reference

1. Ichiro Takasaki, et al. In Silico Screening Identified Novel Small-molecule Antagonists of PAC1 Receptor. J Pharmacol Exp Ther. 2018 Apr;365(1):1-8.?
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