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PA-8

Chemical Structure : PA-8

CAS No.: 878437-15-1

PA-8 (PAC1 antagonist PA-8)

Catalog No.: PC-72883Not For Human Use, Lab Use Only.

PA-8 (PAC1 antagonist PA-8) is a potent, specific small molecule antagonist of PACAP type I (PAC1) receptor.

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Purity & Documentation Purity: >98% (HPLC) Select Batch:

Biological Activity

PA-8 (PAC1 antagonist PA-8) is a potent, specific small molecule antagonist of PACAP type I (PAC1) receptor.
PA-8 (1 nM) significantly and dose dependently attenuated PACAP (1 nM)-induced CREB phosphorylation in the CHO cells expressing PAC1, but not CHO cells expressing VPAC1, or VPAC2 receptors.
PA-8 also dose dependently inhibited PACAP-induced cAMP elevation with an IC50 of 2 nM.
PA-8 blocked PACAP-induced aversive responses and mechanical allodynia in mice.

Physicochemical Properties

M.Wt 342.36
Formula C17H18N4O4
Appearance Solid
CAS No.
Storage
Solide Powder
-20°C 12 Months; 4°C 6 Months
In Solvent
-80°C 6 Months; -20°C 6 Months
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Solubility

10 mM in DMSO

Chemical Name/SMILES

5-(4-(Allyloxy)-3-methoxyphenyl)-2-amino-5,8-dihydropyrido[2,3-d]pyrimidine-4,7(3H,6H)-dione

References

1. Takasaki I, et al. J Pharmacol Exp Ther. 2018 Apr;365(1):1-8.

2. Takasaki I, et al. J Pharmacol Sci. 2019 Feb;139(2):129-132.

3. Shibato J, et al. Neural Plast. 2021 Aug 7;2021:2522454.

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