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.
Bulk size, bulk discount!
E-mail: sales@probechem.com
Tech Support: tech@probechem.com
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.
Contact Us
sales@probechem.com
