• 产品描述： Cenerimod (ACT-334441) is a potent, selective and orally active S1P1 receptor modulator, with an EC50 of 1 nM. Cenerimod shows more than 36‐fold selctivity for hS1P1 over hS1P2, hS1P3, hS1P4, and hS1P5 receptor subtypes (EC50s=>10000, 228, 2134, and 36 nM, respectively). Cenerimod can attenuate murine experimental autoimmune encephalomyelitis (EAE) and murine sclerodermatous

• 靶点： S1PR1:1 nM (EC50);S1PR5:36 nM (EC50);S1PR5:228 nM (EC50);S1PR4:2134 nM (EC50)

• 体外研究：
  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

• 体内研究：
  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. Animal Model: Male Wistar rats weighing 294-510 g Dosage: 0.1, 0.3, 1, 3 and 10 mg/kg Administration: A single p.o. Result: Effectively and reversibly reduced the blood lymphocyte counts, with a plateau reached after a single oral dose of 1 mg/kg.

• 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.

• 溶解性： Soluble  in  DMSO

• 保存条件： 2-8℃

• 配置溶液浓度参考：
  

  	1mg	5mg	10mg
  1 mM	2.205 ml	11.025 ml	22.049 ml
  5 mM	0.441 ml	2.205 ml	4.41 ml
  10 mM	0.22 ml	1.102 ml	2.205 ml
  50 mM	0.044 ml	0.22 ml	0.441 ml

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本计算器可帮助您计算出特定溶液中溶质的质量、溶液浓度和体积之间的关系，公式为：

质量 (mg) = 浓度 (mM) x 体积 (mL) x 分子摩尔量 (g/mol)

• pg ng μg mg g kg =
  fM pM nM μM mM M *
  nL μL mL L *