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- 详细信息
- 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-334441
- 库存:
货期:1-2天
- 供应商:
MedChemExpress LLC
- CAS号:
1262414-04-9
- 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: | ¥698.0 |
|---|---|---|---|
| 规格: | 1 mg | 产品价格: | ¥310.0 |
| 规格: | 5 mg | 产品价格: | ¥700.0 |
| 规格: | 10 mg | 产品价格: | ¥1120.0 |
| 规格: | 25 mg | 产品价格: | ¥2400.0 |
| 规格: | 50 mg | 产品价格: | ¥3840.0 |
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Cenerimod
CAS No. : 1262414-04-9
MCE 国际站:Cenerimod
产品活性:Cenerimod (ACT-334441) 是一种有效,选择性和具有口服活性的 S1P1 受体调节剂,EC50 值为 1 nM。Cenerimod 对 hS1P1 的选择性比 hS1P2,hS1P3,hS1P4 和 hS1P5 受体亚型 (EC50s=>10000,228,2134 和 36 nM) 高出 36 倍以上。Cenerimod 可减轻鼠类实验性自身免疫性脑脊髓炎 (EAE)和鼠类硬皮病。
研究领域:GPCR/G Protein
作用靶点:LPL Receptor
In Vitro: Cenerimod is a highly potent S1P1 receptor agonists in (35S)-GTPγS assays using HUVEC cell membrane preparations, with an EC50 of 2 nM.
Cenerimod activates G protein and increases Ca2+ signaling in CHO cells, with EC50s of 1 nM and 124 nM, respectively.
Cenerimod (5 μM; 24 h) inhibits collagen production in fibroblasts.
In Vivo: Cenerimod (0.1-10 mg/kg; a single p.o.) reversibly reduces the number of circulating lymphocytes in a dose-dependent manner in rats.
Cenerimod (6 mg/kg/day for 30 days; p.o.) attenuates disease in a mouse experimental autoimmune encephalitis (EAE) model.
Cenerimod (10 mg/kg/day for 42 days; p.o.) attenuates skin and lung fibrosis in Scl-cGVHD mice.
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