TY-52156

TY-52156 is an effective and selective S1P3 receptor antagonist (Ki: 110 nM) . TY-52156 displays submicromolar potency and a high degree of selectivity for the S1P3 receptor. TY-52156 inhibits the S1P3 receptor-dependent increase in [Ca2+]i. TY-52156 (10 μM; 10 min) inhibits S1P-induced p44/p42 MAPK phosphorylation.After oral administration in vivo, TY-52156 (10 mg/kg, 30 mg/kg; p.o.) inhibits S1P3 receptor-induced bradycardia.