MrgprX2 antagonist-10 is a potent MRGPRX2 antagonist. MrgprX2 antagonist-10 inhibits MRGPRX2 -mediated accumulation and mast cell degranulation ( IC50 < 100 nM), thereby blocking mast cell activation. MrgprX2 antagonist-10 can be used in research on MRGPRX2-related inflammatory and allergic diseases [1].
In Vitro, MrgprX2 antagonist-10 (Example 218) (15 min pre-incubation + 60 min stimulation) shows inhibitory activity against IP1 accumulation in hMRGPRX2-overexpressing HEK293 cells, with an activity grade of "+++" (IC50 < 100 nM)[1]. MrgprX2 antagonist-10 (15 min pre-incubation + 30 min stimulation) shows inhibitory activity against β-hexosamine release in LAD2 human mast cells, with an activity grade of "+++" (IC50 < 100 nM)[1].
References:
[1]. Steven J., et al. Mrgprx2 antagonists and methods of use thereof. WO2024226914A2.
In Vitro, MrgprX2 antagonist-10 (Example 218) (15 min pre-incubation + 60 min stimulation) shows inhibitory activity against IP1 accumulation in hMRGPRX2-overexpressing HEK293 cells, with an activity grade of "+++" (IC50 < 100 nM)[1]. MrgprX2 antagonist-10 (15 min pre-incubation + 30 min stimulation) shows inhibitory activity against β-hexosamine release in LAD2 human mast cells, with an activity grade of "+++" (IC50 < 100 nM)[1].
References:
[1]. Steven J., et al. Mrgprx2 antagonists and methods of use thereof. WO2024226914A2.