S1P1 agonist III

S1P1 Agonist III is a potent and orally active S1P1 agonist with EC50 of 18 nM; no activity on S1P3. IC50 value: 18 nM (EC50) [1] Target: S1P1 agonist When dosed orally at 1 and 3 mg/kg, the azahydroxymethyl analogue 22 (HY-12835) achieved statistically significant lowering of circulating blood lymphocytes 24 h postdose. In rats, a dose-proportional increase in exposure was measured when 22 (HY-12835) was dosed orally at 2 and 100 mg/kg. 22 displayed excellent pharmacokinetic parameters with low clearance (CL = 0.11 L/h/kg), long mean residence time (40 h), and good oral bioavailability (F = 67%) .