Bioactivity | Icanbelimod (S1p receptor agonist 1) is a potent and orally active?S1P?receptor agonist, exhibits an activity of inducing S1P1 internalization (EC50=9.83 nM). Icanbelimod has the potential for the study of arthritis and EAE (experimental autoimmune encephalitis). Icanbelimod is extracted from patent WO2015039587A1, Compound 2[1]. | ||||||||||||
Target | EC50: 9.83 nM (S1P1 internalization) | ||||||||||||
In Vivo | Icanbelimod (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].Icanbelimod (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].Icanbelimod (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]. Animal Model: | ||||||||||||
Name | Icanbelimod | ||||||||||||
CAS | 1514888-56-2 | ||||||||||||
Formula | C23H24FN3O3 | ||||||||||||
Molar Mass | 409.45 | ||||||||||||
Appearance | Solid | ||||||||||||
Transport | Room temperature in continental US; may vary elsewhere. | ||||||||||||
Storage |
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Reference | [1]. Zhenwei, et al. Immune adjustment compound, use thereof and pharmaceutical composition comprising same. Patent WO2015039587A1 |