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
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M.Wt
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218.30
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Formula
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C13H18N2O
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Appearance
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Solid
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CAS No.
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Storage
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- Solide Powder
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-20°C 12 Months; 4°C 6 Months
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- In Solvent
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-80°C 6 Months; -20°C 6 Months
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Shipping
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Solubility
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10 mM in DMSO
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Chemical Name/SMILES
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2,2,3,3-tetramethyl-N-(pyridin-2-yl)cyclopropane-1-carboxamide
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References
1. Macphee CH, et al. Front Immunol. 2024 Oct 18;15:1433982.
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