Description
RP 001 is a potent sphingosine-1-phosphate receptor 1 (S1P
1) agonist (EC
50 = 9 pM). It is competitive with W146 , a selective S1P
1 antagonist, and induces internalization and polyubiquitination of S1P
1 in a dose-dependent manner. RP 001 induces dose-dependent lymphopenia in mice (EC
50 = 0.03 mg/kg). It reduces S1P
1-EGFP expression
ex vivo on lymphocytes in the isolated lymph node of
Edg1eGFP/eGFP mice but has no effect
in vivo. RP 001 also completely inhibits
M. stadtmanae (MSS) rechallenge-induced enlargement of B cell-rich tertiary lymphoid tissues (TLTs) and reduces neutrophil accumulation in the airways of a mouse model of experimental hypersensitivity pneumonitis.
