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首页-小分子抑制剂&激动剂-GPCR-Vasoactive intestinal peptide receptor (VIPR)-PA-8
PA-8

Chemical Structure : PA-8

CAS No.: 878437-15-1

PA-8 (PAC1 antagonist PA-8)

货号: 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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纯度 & COA & 质检文件 纯度: >98% (HPLC) Select Batch:

生物&药学活性

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.

物理化学性质&存储条件

分子量 342.36
分子式 C17H18N4O4
外观性状 Solid
CAS No.
储存条件
固体粉末
-20°C 12 个月; 4°C 6 个月
配置液
-80°C 6 个月; -20°C 6 个月
Shipping
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

参考文献

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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