MrgprX2 antagonist-11 is a potent MrgprX2 antagonist. MrgprX2 antagonist-11 inhibits MrgprX2 -mediated accumulation and mast cell degranulation ( IC50 < 100 nM), thereby blocking mast cell activation. MrgprX2 antagonist-11 can be used in research on MrgprX2-related inflammatory and allergic diseases [1].
In Vitro, MrgprX2 antagonist-11 (Example 53) (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-11 (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]. The structure of MrgprX2 antagonist-11 is confirmed by 1H NMR and LCMS. The measured MS (ESI) m/z = 494.05 [M+H]+, which is consistent with the theoretical value[1].
References:
[1]. Steven J., et al. Mrgprx2 antagonists and methods of use thereof. WO2024226914A2.
In Vitro, MrgprX2 antagonist-11 (Example 53) (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-11 (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]. The structure of MrgprX2 antagonist-11 is confirmed by 1H NMR and LCMS. The measured MS (ESI) m/z = 494.05 [M+H]+, which is consistent with the theoretical value[1].
References:
[1]. Steven J., et al. Mrgprx2 antagonists and methods of use thereof. WO2024226914A2.