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首页-小分子抑制剂&激动剂-GPCR-Neuropeptide Y Receptor-NPSR1 antagonist Compound 6
NPSR1 antagonist Compound 6

Chemical Structure : NPSR1 antagonist Compound 6

CAS No.: 3113770-74-1

NPSR1 antagonist Compound 6

货号: PC-28044Not For Human Use, Lab Use Only.

NPSR1 antagonist Compound 6 is a potent, selective and peripherally biased neuropeptide S receptor 1 (NPSR1, GPR154) with IC50 of 0.35 nM and 0.15 nM in calcium assay against NPSR1-A and NPSR1-B, respectively.

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纯度 & COA & 质检文件 纯度: >98% (HPLC)

生物&药学活性

NPSR1 antagonist Compound 6 is a potent, selective and peripherally biased neuropeptide S receptor 1 (NPSR1, GPR154) with IC50 of 0.35 nM and 0.15 nM in calcium assay against NPSR1-A and NPSR1-B, respectively.
NPSR1 antagonist Compound 6 has IC50 of 0.22 nM in the cAMP assay.
NPSR1 antagonist Compound 6 effectively inhibits the expression of the NPS-induced markers without affecting expression of non-NPS induced genes in NPSR1-A expressing fibroblasts.
NPSR1 antagonist Compound 6 (10 mg/kg) reduces TNF-α and altered macrophage populations in zymosan-induced inflammatory mouse model.

物理化学性质&存储条件

分子量 528.69
分子式 C30H42F2N4O2
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-((4,4-difluoro-1-(4-methylpiperazin-1-yl)cyclohexyl)methyl)-N-((1-methyl-2-oxo-1,2-dihydroquinolin-3-yl)methyl)cyclohexanecarboxamide

参考文献

1. Berger KJ, et al. Bioorg Med Chem Lett. 2025 Dec 1;128:130353.

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