Ponesimod

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Chemical Structure| 854107-55-4 同义名 : ACT-128800
CAS号 : 854107-55-4
货号 : A257238
分子式 : C23H25ClN2O4S
纯度 : 99%+
分子量 : 460.97
MDL号 : MFCD18207776
存储条件：

Pure form Sealed in dry, 2-8°C

In solvent -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 105 mg/mL(227.78 mM)，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO
生物活性
描述 S1P is a signaling lipid that regulates many cellular processes in mammals[3]. Ponesimod is a potent, selective, and orally active S1P(1) receptor agonist (IC50=6nM) selected for clinical development[4]. Ponesimod activated S1P(1)-mediated signal transduction with high potency (EC50-5.7nM) and selectively. Oral administration of ponesimod (3-100mg/kg) to rats led to a dose-dependent decrease of blood lymphocyte count. Ponesimod (30 mg/kg) also prevents footpad swelling in a rat model of adjuvant-induced arthritis[5].
临床研究
NCT号 适应症或疾病 临床期 招募状态 预计完成时间 地点
NCT01208090 Psoriasis Phase 2 Completed - -
NCT01006265 Multiple Sclerosis Phase 2 Completed - -
NCT02223832 Healthy Phase 1 Completed - United States, Hawaii ... 展开 >> Hawaii Clinical Research Center Honolulu, Hawaii, United States, 96813 收起 <<
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

2.17mL

0.43mL

0.22mL

10.85mL

2.17mL

1.08mL

21.69mL

4.34mL

2.17mL
参考文献

[1]D'Ambrosio D, Freedman MS, et al. Ponesimod, a selective S1P1 receptor modulator: a potential treatment for multiple sclerosis and other immune-mediated diseases. Ther Adv Chronic Dis. 2016 Jan;7(1):18-33.

[2]Piali L, Froidevaux S, et al. The selective sphingosine 1-phosphate receptor 1 agonist ponesimod protects against lymphocyte-mediated tissue inflammation. J Pharmacol Exp Ther. 2011 May;337(2):547-56.

[3]Bryan AM, Del Poeta M. Sphingosine-1-phosphate receptors and innate immunity. Cell Microbiol. 2018 May;20(5):e12836.

[4]Bolli MH, Abele S, Binkert C, et al. 2-imino-thiazolidin-4-one derivatives as potent, orally active S1P1 receptor agonists. J Med Chem. 2010;53(10):4198-4211.

[5]Piali L, Froidevaux S, Hess P, et al. The selective sphingosine 1-phosphate receptor 1 agonist ponesimod protects against lymphocyte-mediated tissue inflammation. J Pharmacol Exp Ther. 2011;337(2):547-556.