| 产品描述: | TY-52156 is a potent and selective S1P3 receptor antagonist with a Ki value of 110 nM |
| 靶点: |
Ki: 110 nM (S1P3) |
| 体外研究: |
TY-52156 抑制 [Ca2+]i 中 S1P3 受体依赖性增加。 TY-52156 对 S1P3 受体显示出亚微摩尔级效力和高度选择性。 TY-52156 (10 μM;10 min) 抑制 S1P 诱导的 p44/p42 MAPK 磷酸化。 Western Blot Analysis Cell Line: Chinese hamster ovary K1 cells Concentration: 10 μM Incubation Time: 10 min Result: Inhibited S1P-induced p44/p42 MAPK phosphorylation. |
| 体内研究: |
TY-52156 (10 mg/kg,30 mg/kg;口服) 在体内口服给药后抑制 S1P3 受体诱导的心动过缓。Animal Model: Male SD rats (290–340 g)Dosage: 10 mg/kg, 30 mg/kgAdministration: Oral administrationResult: Inhibited S1P3 receptor-induced bradycardia after oral administration in vivo. |
| 参考文献: |
1. Murakami A, et al. Sphingosine 1-phosphate (S1P) regulates vascular contraction via S1P3 receptor: investigation based on a new S1P3 receptor antagonist. Mol Pharmacol. 2010 Apr;77(4):704-13. |
| 溶解性: |
Soluble in DMSO |
| 保存条件: |
-80℃(运输条件:冰袋低温运输) |
| 配置溶液浓度参考: |
|
1mg |
5mg |
10mg |
| 1 mM |
2.745 ml |
13.726 ml |
27.452 ml |
| 5 mM |
0.549 ml |
2.745 ml |
5.49 ml |
| 10 mM |
0.275 ml |
1.373 ml |
2.745 ml |
| 50 mM |
0.055 ml |
0.275 ml |
0.549 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。 |