TC-G 1006

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 agonistWhen 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%).

Signaling Pathways >> GPCR/G Protein >> LPL Receptor

Research Areas >> Inflammation/Immunology

[1]. Harrington PE, et al. Optimization of a Potent, Orally Active S1P1 Agonist Containing a Quinolinone Core. ACS Med Chem Lett. 2011 Nov 23;3(1):74-8.

Ki16425 | Siponimod | AM966 | Ozanimod | BMS-986020 | LPA2 antagonist 1 | TY-52156 | AM095 | Etrasimod | ACT-334441 | Ponesimod | Amiselimod hydrochloride | S1p receptor agonist 1 | ONO-7300243