PA-8

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].

Product Specifications

CAS Number

[878437-15-1]

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.