S1p receptor agonist 1 是一种有效的口服活性 S1P receptor 激动剂，具有诱导 S1P1 内化的活性 (EC₅₀=9.83 nM)。S1p receptor agonist 1 有潜力用于研究关节炎和 EAE (实验性自身免疫性脑炎) 的相关研究。S1p receptor agonist 1 是专利 WO2015039587A1 中的化合物 2。

S1p receptor agonist 1 is a potent and orally active S1P receptor agonist, exhibits an activity of inducing S1P1 internalization (EC 50 =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.

Solid

EC50: 9.83 nM (S1P1 internalization)

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.
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.
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 mann

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Powder -20°C 3 years；4°C 2 years

[1]. Zhenwei, et al. Immune adjustment compound, use thereof and pharmaceutical composition comprising same. Patent WO2015039587A1

In Vitro: DMSO : 6.8 mg/mL (16.61 mM; Need ultrasonic and warming)配制储备液