| 产品描述： | Etrasimod (APD334) is a potent, selective and orally available antagonist of the sphingosine-1-phosphate-1 (S1P1) receptor with an IC50 value of 1.88 nM in CHO cells |
| 靶点： |
IC50: 1.88 nM (S1P1);S1PReceptor; LPLReceptor |
| 体外研究： |
APD334 is a structurally novel, selective, functional antagonist of S1P1. In CHO cells expressing HA tagged S1P1, APD334 is found to have an IC50 value of 1.88 nM. Moderate agonism at human S1P4 and S1P5 is observed but is reduced relative to S1P1, both in terms of potency and efficacy. APD334 is devoid of any agonism or antagonism at human S1P2 and S1P3. APD334 achieves good central exposure following oral dosing and possesses a favorable pharmacokinetic profile in multiple preclinical species. S1P1 activity is maintained in mice (EC50=0.44 nM), rats (EC50=0.32 nM), dogs (EC50=0.34 nM) and monkeys (EC50=0.32 nM) |
| 体内研究： |
APD334 has a relatively low systemic clearance (<4% of hepatic blood flow) and high Cmax across all species. In both dog and monkey a significant decrease in volume of distribution (Vss) is observed relative to rodent. Oral bioavailability is in the range of 40–100%, and the terminal phase half-life varied from 6 h in monkey, to as long as 29 h in dog. Rat and monkey t1/2 values for siponimod (another S1P1 modulator currently in human trials) have been disclosed and are 6 and 19 h, respectively |
| 参考文献： |
1. Buzard DJ, et al. Discovery of APD334: Design of a Clinical Stage Functional Antagonist of the Sphingosine-1-phosphate-1 Receptor. ACS Med Chem Lett. 2014 Nov 4;5(12):1313-7. |
| 溶解性： |
soluble in DMSO |
| 保存条件： |
-20℃ |
| 配置溶液浓度参考： |
|
1mg |
5mg |
10mg |
| 1 mM |
2.186 ml |
10.929 ml |
21.859 ml |
| 5 mM |
0.437 ml |
2.186 ml |
4.372 ml |
| 10 mM |
0.219 ml |
1.093 ml |
2.186 ml |
| 50 mM |
0.044 ml |
0.219 ml |
0.437 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
危险品化学品经营许可证（不带存储）
营业执照(三证合一)
北京