|
产品描述： Ponesimod (ACT-128800) is a potent, selective and orally active agonist of S1P1, with an IC50 of 6 nM in a radioligand binding assay. Ponesimod activates S1P1-mediated signal transduction with high potency (EC50=5.7 nM). Ponesimod can protect against lymphocyte-mediated tissue inflammation |
|
靶点：
S1PR1：6 nM (IC50)；S1PR3：2068 nM (IC50)；S1PR4：1956 nM (IC50)；S1PR5：142 nM (IC50);S1PReceptor; LPLReceptor |
体内研究：
Ponesimod (30 and 175 mg/kg; once daily p.o. for 8 d) prevents delayed-type hypersensitivity in mice. Ponesimod (30 mg/kg by gavage 3 h before and 6 h after adjuvant injection followed by 100 mg/kg/day by administration as food admix for 18 days) prevents adjuvant-induced arthritis in rats. Ponesimod (0.3-100 mg/kg; a single oral gavage) causes a dose-dependent reduction in lymphocyte count, with a plateau effect being reached at 3 mg/kg in rats. Ponesimod (100 mg/kg; once daily oral gavage for 7 d) results in a lymphocyte count reduction to 1900 lymphocytes/μL, and this effect is maintained over the entire 7 days studies. Lymphocyte count returned to baseline levels within 48 h after discontinuation of dosing. |
参考文献：
1. Bolli MH, et al. 2-imino-thiazolidin-4-one derivatives as potent, orally active S1P1 receptor agonists. J Med Chem. 2010 May 27;53(10):4198-211. 2. Piali L, 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. Brossard P, et al. Pharmacokinetics and pharmacodynamics of ponesimod, a selective S1P1 receptor modulator, in the first-in-human study. Br J Clin Pharmacol. 2013 Dec;76(6):888-96. |
|
溶解性：
DMSO : ≥ 100 mg/mL (216.93 mM) |
|
保存条件：
2-8℃ |
配置溶液浓度参考：
|
1mg |
5mg |
10mg |
| 1 mM |
2.169 ml |
10.847 ml |
21.693 ml |
| 5 mM |
0.434 ml |
2.169 ml |
4.339 ml |
| 10 mM |
0.217 ml |
1.085 ml |
2.169 ml |
| 50 mM |
0.043 ml |
0.217 ml |
0.434 ml |
|
| 注意： |
部分产品我司仅能提供部分信息，我司不保证所提供信息的权威性，仅供客户参考交流研究之用。 |
上海工商
北京