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首页-小分子抑制剂&激动剂-GPCR-Vasoactive intestinal peptide receptor (VIPR)-PA-915
PA-915

Chemical Structure : PA-915

CAS No.: 2305204-24-2

PA-915 (PA915)

货号: PC-49382Not For Human Use, Lab Use Only.

PA-915 (PA915) is a small-molecule, non-peptide antagonist of the PACAP type I (PAC1) receptor, inhibits PACAP (1 nM)-induced phosphorylation of CREB in PAC1/CHO cells with IC50 of <10 pM.

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

生物&药学活性

PA-915 (PA915) is a small-molecule, non-peptide antagonist of the PACAP type I (PAC1) receptor, inhibits PACAP (1 nM)-induced phosphorylation of CREB in PAC1/CHO cells with IC50 of <10 pM.
PA-915 is more potent than PA-9 on the PACAP-induced phosphorylation of CREB in the PAC1/CHO cells.
PA-915 inhibited both pituitary adenylate cyclase-activating polypeptide (PACAP) and spinal nerve ligation-induced mechanical allodynia.
PA-915 also showed anti-allodynic effects following oral administration.

物理化学性质&存储条件

分子量 372.813
分子式 C17H17ClN6O2
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

N-(2-(1H-imidazol-4-yl)ethyl)-1-(7-chloro-1H-indazol-3-yl)-5-oxopyrrolidine-3-carboxamide

参考文献

1. Ichiro Takasaki, et al. Eur J Med Chem. 2020 Jan 15;186:111902.

2. Yusuke Shintani, et al. Biochem Biophys Res Commun. 2022 Nov 26;631:146-151.

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