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首页-小分子抑制剂&激动剂-GPCR-Mas-related G protein-coupled receptor (MRGPR)-MRGPRX2 antagonist Compound A
MRGPRX2 antagonist Compound A

Chemical Structure : MRGPRX2 antagonist Compound A

CAS No.: 329059-49-6

MRGPRX2 antagonist Compound A

货号: PC-23467Not For Human Use, Lab Use Only.

MRGPRX2 antagonist Compound A is a potent, selective MRGPRX2 antagonist with IC50 of 50 nM for inhibition of cortistatin 14-mediated MRGPRX2 activation.

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纯度 & COA & 质检文件 纯度: >98% (HPLC)

生物&药学活性

MRGPRX2 antagonist Compound A is a potent, selective MRGPRX2 antagonist with IC50 of 50 nM for inhibition of cortistatin 14-mediated MRGPRX2 activation.
Compound A exhibits insurmountable inhibition of Substance P–stimulated LAD2 mast cell degranulation.
Compound A exhibits concentration-dependent inhibition of Cortistatin 14–mediated degranulation with IC50 of 22.8 nM.
Compound A demonstrates excellent selectivity in off-target screening for in vitro secondary pharmacology that included GPCRs, ion channels, and enzymes as targets, including MRGPRX1.
Compound A inhibits substance P–stimulated LAD2 degranulation with IC50 of 32.4 nM.

物理化学性质&存储条件

分子量 218.30
分子式 C13H18N2O
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

2,2,3,3-tetramethyl-N-(pyridin-2-yl)cyclopropane-1-carboxamide

参考文献

1. Macphee CH, et al. Front Immunol. 2024 Oct 18;15:1433982.

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