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MRGPRX2 antagonist Compound B

Chemical Structure : MRGPRX2 antagonist Compound B

CAS No.: 2767111-67-9

MRGPRX2 antagonist Compound B

Catalog No.: 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.

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Purity & Documentation Purity: >98% (HPLC)

Biological Activity

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.

Physicochemical Properties

M.Wt 491.45
Formula C23H21F4N5O3
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

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

References

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

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