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Icanbelimod

MCE China：Icanbelimod

Brand：MedChemExpress (MCE)

Cat. No.HY-101265

CAS：1514888-56-2

Synonyms：S1p receptor agonist 1

Purity：99.95%

Storage：Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year

Shipping：Room temperature in continental US; may vary elsewhere.

Description：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.

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].

IC50 & Target：EC50: 9.83 nM (S1P1 internalization)[1] 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]. MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model: Lewis rats[1]

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References：

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