MRGPRX2 antagonist Compound B

Chemical Structure : MRGPRX2 antagonist Compound B

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货号: PC-23468Not For Human Use, Lab Use Only.

MRGPRX2 antagonist Compound B is a potent, selective MRGPRX2 antagonist with IC50 of 2.9 nM for inhibition of cortistatin 14-mediated MRGPRX2 activation.

规格	价格	库存	数量
25 mg		Get quote
50 mg		Get quote
100 mg		Get quote

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生物&药学活性

MRGPRX2 antagonist Compound B is a potent, selective MRGPRX2 antagonist with IC50 of 2.9 nM for inhibition of cortistatin 14-mediated MRGPRX2 activation.
Compound B exhibits insurmountable inhibition of Substance P–stimulated LAD2 mast cell degranulation.
Compound B exhibits concentration-dependent inhibition of Cortistatin 14–mediated degranulation with IC50 of 1.0 nM.
Compound B demonstrates excellent selectivity in off-target screening for in vitro secondary pharmacology that included GPCRs, ion channels, and enzymes as targets, including MRGPRX1.
Compound B inhibits substance P–stimulated LAD2 degranulation with IC50 of 1.8 nM.

物理化学性质&存储条件

分子量	491.45
分子式	C23H21F4N5O3
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	4-[(3S)-1-[(1S)-1-{[5-(2,4-difluorophenoxy)pyrazin-2-yl]carbamoyl}ethyl]-4,4-difluoropiperidin-3-yl]pyridin-1-ium-1-olate

参考文献

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