Cenerimod|1262414-04-9|(ACT-334441)-陌孚医药/Medlife

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Cenerimod (Synonyms: ACT-334441)

目录号: PL06780 纯度: ≥98.0%

CAS No. :1262414-04-9

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中文名称	Cenerimod
英文名称	Cenerimod
英文别名	Cenerimod;ACT-334441;ACT334441
Cas No.	1262414-04-9
分子式	C₂₅H₃₁N₃O₅
分子量	453.53
包装储存	Powder -20°C 3 years；4°C 2 years

产品详情

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 16 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。

生物活性

Cenerimod (ACT-334441) is a potent, selective and orally active S1P1 receptor modulator, with an EC 50 of 1 nM. Cenerimod shows more than 36‐fold selctivity for hS1P1 over hS1P2, hS1P3, hS1P4, and hS1P5 receptor subtypes (EC 50 s=>10000, 228, 2134, and 36 nM, respectively). Cenerimod can attenuate murine experimental autoimmune encephalomyelitis (EAE) and murine sclerodermatous.

性状

Solid

IC50 & Target[1][2]

S1PR1 1 nM (EC50) S1PR5 36 nM (EC50

体外研究(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 Ca signaling in CHO cells, with EC50s of 1 nM and 124 nM, respectively.
Cenerimod (5 μM; 24 h) inhibits collagen production in fibroblasts. has not independently confirmed the accuracy of these methods. They are for reference only.

体内研究(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. has not independently confirmed the accuracy of these methods. They are for reference only.

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Powder -20°C 3 years；4°C 2 years

ClinicalTrial

参考文献

[1]. Piali L, et, al. Cenerimod, a novel selective S1P 1 receptor modulator with unique signaling properties. Pharmacol Res Perspect. 2017 Dec;5(6):e00370.
[2]. Kano M, et, al. Attenuation of murine sclerodermatous models by the selective S1P 1 receptor modulator cenerimod. Sci Rep. 2019 Jan 24;9(1):658.

溶解度数据	In Vitro: DMSO : ≥ 100 mg/mL (220.49 mM)配制储备液

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Data Sheet

1：一般建议：溶解度为Medlife测试数据，可能与文献描述存在差异。这是由于生产工艺和批次不同产生的正常现象。为了使其更好的溶解，请用37℃加热试管并在超声波水浴中震动片刻。不同批次产品溶解度各有差异，仅做参考，具体以实验方案为准。

2：储存条件：粉末-20°C一般情况可以保存3年，溶于溶剂-80°C一般情况可以保存1年。不同产品及不同批次产品可能存在差异，请细致阅读产品信息，并辅助参考相关文献描述。

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