S1P1 agonist III

S1P1 agonist III is an orally active hS1P1 agonist with an EC₅₀ value of 18 nM. S1P1 agonist III shows limited activity against hS1P3. S1P1 agonist III can be used in the research of multiple sclerosis^[1]. In Vitro:S1P1 agonist III induces potent internalization of hS1P₁ receptors in U2OS cells with an EC₅₀ of 0.018 μM^[1].
S1P1 agonist III shows minimal agonist activity at hS1P₃ receptors in transfected CHO-K1 cells, with an EC₅₀ greater than 25 μM^[1].
S1P1 agonist III exhibits moderate permeability across LLC-PK1 porcine proximal tubule cells with no significant efflux, as shown by a P_app of 2.5 × 10^-6 cm/s and an efflux ratio of 1.0^[1].
S1P1 agonist III binds to 91.7% of rat plasma proteins under equilibrium conditions^[1].
S1P1 agonist III is highly stable in rat liver microsomes, with an intrinsic clearance of less than 14 μL/min/mg microsomal protein^[1]. In Vivo:S1P1 agonist III (compound 22) (1-3 mg/kg; p.o.; single dose) produces statistically significant circulating blood lymphocyte reduction in female Lewis rats at 24 hours, with the 3 mg/kg dose causing an 88% reduction^[1].