878437-15-1
878437-15-1
Chemical Structure
PA-8
- CAS No.: 878437-15-1
- Formula:C17H18N4O4
- Molecular Weight:342.35
IUPAC Name: 5-(4-(allyloxy)-3-methoxyphenyl)-2-amino-5,8-dihydropyrido[2,3-d]pyrimidine-4,7(3H,6H)-dione
InChIKey: DCSWTWUTSKSXOV-UHFFFAOYSA-N
SMILES: O=C1C(C(C2=CC=C(OCC=C)C(OC)=C2)CC(N3)=O)=C3N=C(N)N1
Biological Activity: 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].
| Cat. No. | Product Name | Purity | Description | Pricing | |||||||||||||||||||
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PA-8 | 97.00% | 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. | ||||||||||||||||||||
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References
- [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. [Content Brief]
- [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. [Content Brief]
