产品
编 号：F102678
分子式：C25H31N3O5
分子量：453.53
分子式：C25H31N3O5
分子量：453.53
产品类型
规格
价格
是否有货
10mM*1mL in DMSO
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5mg
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10mg
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25mg
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50mg
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100mg
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结构图
CAS No: 1262414-04-9
产品详情
生物活性：
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.
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.
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.
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.
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.
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.
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