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Ponesimod

CAS No. : 854107-55-4

MCE 站：Ponesimod

产品活性：Ponesimod (ACT-128800) 是一种有效的，具有选择性和口服活性的 S1P₁ 的激动剂，在放射性配体结合试验中的 IC₅₀ 值为 6 nM。Ponesimod 可高效激活 S1P₁ 介导的信号转导 (EC₅₀=5.7 nM)。Ponesimod 可以预防淋巴细胞介导的组织炎症。

研究领域：GPCR/G Protein

作用靶点：LPL Receptor

In Vitro: Ponesimod activates human S1P_1-5 receptors with EC₅₀s of 5.7, >10000, 105, 1108 and 59.1 nM respectively in GTPγS binding assay.
Ponesimod activates S1P₁ receptors with EC₅₀s of 5.7, 1.9, and 1.4 nM for human, rat, and mouse S1P receptors respectively.

In Vivo: Ponesimod (30 and 175 mg/kg; once daily p.o. for 8 d) prevents delayed-type hypersensitivity in mice.
Ponesimod (30 mg/kg by gavage 3 h before and 6 h after adjuvant injection followed by 100 mg/kg/day by administration as food admix for 18 days) prevents adjuvant-induced arthritis in rats.
Ponesimod (0.3-100 mg/kg; a single oral gavage) causes a dose-dependent reduction in lymphocyte count, with a plateau effect being reached at 3 mg/kg in rats.
Ponesimod (100 mg/kg; once daily oral gavage for 7 d) results in a lymphocyte count reduction to 1900 lymphocytes/μL, and this effect is maintained over the entire 7 days studies. Lymphocyte count returned to baseline levels within 48 h after discontinuation of dosing.

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