RP-001 hydrochloride is a picomolar short-acting S1P1 (EDG1) selective agonist, with an EC50 of 9 pM. RP-00 hydrochloride induces internalization and polyubiquitination of S1P1. RP-001 hydrochloride has little activity on S1P2-S1P4 and only moderate affinity for S1P5.
体外研究:
RP-001 hydrochloride elicits dose-dependent lymphopenia of CD4+ T cells. RP-001 hydrochloride induces acute lymphopenia with rapid recovery to untreated levels.