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- MedChemExpress(MCE)
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- 2025年12月05日
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- 技术资料
- 保存条件：
Powder: -20°C, 3 years; 4°C, 2 years.In solvent: -80°C, 6 months; -20°C, 1 month.
- 英文名：
ACT-128800
- 库存：
货期：1-2天
- 供应商：
MedChemExpress LLC
- CAS号：
854107-55-4
- 规格：
10 mM * 1 mL/1 mg/5 mg/10 mg/25 mg/50 mg
| 规格： | 10 mM * 1 mL | 产品价格： | ￥1014.0 |
|---|---|---|---|
| 规格： | 1 mg | 产品价格： | ￥454.0 |
| 规格： | 5 mg | 产品价格： | ￥1000.0 |
| 规格： | 10 mg | 产品价格： | ￥1600.0 |
| 规格： | 25 mg | 产品价格： | ￥2788.0 |
| 规格： | 50 mg | 产品价格： | ￥4163.0 |
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Ponesimod
CAS No. : 854107-55-4
MCE 国际站：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 S1P1-5 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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