GnRH-R antagonist 1 (compound 21a) is an orally safe and membrane-permeable GnRH-R antagonist with high binding affinity (IC50=0.57 nM) and potent in vitro antagonistic activity (IC50=2.18 nM). GnRH-R antagonist 1 can be used in studies of advanced prostate cancer and premature LH peaks preventing[1].
GPVI antagonist 1 (compound 5) is a glycoprotein VI (GPVI) platelet receptor antagonist. GPVI antagonist 1 inhibits collagen-induced platelet aggregation with an IC50 of 25.3 μM[1].
MrgprX2 antagonist-1 is an MrgprX2 antagonist extracted from patent WO2021092264A1, example E23. MrgprX2 antagonist-1 can be used for the research of inflammatory disorders of the skin[1].