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MRGPRX2 antagonist Compound A

Chemical Structure : MRGPRX2 antagonist Compound A

CAS No.: 329059-49-6

MRGPRX2 antagonist Compound A

Catalog No.: 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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Purity & Documentation Purity: >98% (HPLC)

Biological Activity

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.

Physicochemical Properties

M.Wt 218.30
Formula C13H18N2O
Appearance Solid
CAS No.
Storage
Solide Powder
-20°C 12 Months; 4°C 6 Months
In Solvent
-80°C 6 Months; -20°C 6 Months
Shipping
Solubility

10 mM in DMSO

Chemical Name/SMILES

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

References

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

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