S1p receptor agonist 1 is a potent and orally active S1P receptoragonist, exhibits an activity of inducing S1P1 internalization (EC₅₀=9.83 nM). S1p receptor agonist 1 has the potential for the study of arthritis and EAE (experimental autoimmune encephalitis). S1p receptor agonist 1 is extracted from patent WO2015039587A1, Compound 2^[1].

EC50: 9.83 nM (S1P1 internalization)^[1]

S1p receptor agonist 1 (oral administration; 0.01 mg/kg-1 mg/kg) at all dose is active, and only a dose of 0.01 mg/kg is required to observe a decrease in the number of peripheral blood lymphocytes by more than 50% and a decrease in the 1 mg/kg dose. Besides, this compound is lymphocyte-specific, which dose not significantly alter the number of peripheral monocytes and other white blood cells in SD rats^[1].
S1p receptor agonist 1 (oral administration; 3 mg/kg; 12 days) is has been proved to block lymphocyte efflux. In the development of type II collagen-induced arthritis in rat model, compound 2 is effective in inhibiting the development of joint swelling in arthritis and joint structure destruction^[1].
S1p receptor agonist 1 (oral administration; 0.3-1mg/kg; 30 days; once daily) inhibits the development of experimental autoimmune encephalitis (EAE) as a dose-dependent manner in mice model^[1].

409.45

Solid

C₂₃H₂₄FN₃O₃

1514888-56-2

Room temperature in continental US; may vary elsewhere.

DMSO : 6.8 mg/mL(16.61 mM;Need ultrasonic and warming)

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