PA-8

• 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[1][2].

• UNSPSC:

  12352005

• Hazard Statement:

  H315, H319, H335, H412

• Target:

  PACAP Receptor

• Type:

  Reference compound

• Related Pathways:

  GPCR/G Protein

• Applications:

  COVID-19-immunoregulation

• Field of Research:

  Inflammation/Immunology; Neurological Disease

• Assay Protocol:

  https://www.medchemexpress.com/pa-8.html

• Purity:

  97.02

• Solubility:

  DMSO : 25 mg/mL (ultrasonic; warming; heat to 60°C)

• Smiles:

  O=C1C(C(C2=CC=C(OCC=C)C(OC)=C2)CC(N3)=O)=C3N=C(N)N1

• Molecular Formula:

  C17H18N4O4

• Molecular Weight:

  342.35

• Precautions:

  H315, H319, H335, H412

• References & Citations:

  [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.|[2]Ichiro Takasaki, et al. The novel small-molecule antagonist of PAC1 receptor attenuates formalin-induced inflammatory pain behaviors in mice. J Pharmacol Sci. 2019 Feb;139 (2) :129-132.

• Shipping Conditions:

  Room Temperature

• Storage Conditions:

  -20°C, 3 years; 4°C, 2 years (Powder)

• Scientific Category:

  Reference compound1

• Clinical Information:

  No Development Reported

• CAS Number:

  [878437-15-1]