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Ozanimod

CAS No. : 1306760-87-1

MCE 站：Ozanimod

产品活性：Ozanimod (RPC-1063) 是一种有效的选择性 S1P₁ 和 S1P₅ 受体激动剂，在[³⁵S]-GTPγS 结合实验中，EC₅₀ 分别为 410 pM 和 11 nM。

研究领域：GPCR/G Protein

作用靶点：LPL Receptor

In Vitro: Ozanimod (RPC1063) is a potent sphingosine-1-phosphate receptor-1 (S1P₁) and receptor-5 (S1P₅) agonist. The EC₅₀ values are subnanomolar for S1P₁ receptors whether measuring inhibition of cAMP generation (160±60 pM) or [³⁵S]-GTPγS binding (410±160 pM). The EC₅₀ value for S1P₅ receptor whether measuring inhibition [³⁵S]-GTPγS binding (11±4.3 nM). Ozanimod demonstrates agonist activity at the S1P₅ receptor [11±4.3 nM and 83% E_max (percentage of maximum stimulation)]. To determine whether Ozanimod induces sustained S1P₁ receptor internalization, S1P₁ receptor-HEK293T cells are incubated with different doses of Ozanimod in the presence of 10 μM cycloheximide to prevent translation of new S1P₁ receptor protein. Cells are analysed after 1 h treatment, or, after the 1 h treatment washed thoroughly to remove Ozanimod and incubated with 1 μM Cycloheximide for a further 24 h. After a 1 h treatment Ozanimod induces significant loss of S1P₁ receptor cell surface expression, similar in magnitude and potency to that seen with FTY720-P-treated cells. Following 1 h of treatment and a 24 h washout period, Ozanimod demonstrates a dose-dependent effect on S1P₁ receptor re-expression on the cell surface, with near complete and sustained loss of cell surface receptor expression at concentrations above 10 nM.

In Vivo: Ozanimod (RPC1063) is specific for S1P₁ and S1P₅ receptors, induces S1P₁ receptor internalization and induces a reversible reduction in circulating B and CCR7⁺ T lymphocytes in vivo. Ozanimod shows high oral bioavailability and volume of distribution, and a circulatory half-life that supports once daily dosing. Oral Ozanimod reduces inflammation and disease parameters in all three autoimmune disease models.

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