生物活性 | |||
---|---|---|---|
描述 | Sphingosine 1-phosphate 3 (S1P3) receptor is distributed on cardiac myocytes and cardiac fibroblasts in vivo and it plays a critical role in cardiovascular physiology, especially pace-making activity. CYM 5541 is a full S1P3-selective agonist, able to reach the maximum level of ERK phosphorylation that was observed with S1P. CYM-5541 has an EC50 of between 72 and 132 nM and exhibits exquisite selectivity over other S1P receptor subtypes in vitro: S1P1 EC50 > 10 μM, S1P2 EC50 > 50 μM, S1P4 EC50 > 50 μM, and S1P5 EC50 > 25 μM[3]. 10 nM of CYM5541 promotes the proliferation and attenuates apoptosis of bone marrow (BM)-derived Endothelial progenitor cells induced by H2O2Wang H, Huang H, Ding SF. Sphingosine-1-phosphate promotes the proliferation and attenuates apoptosis of Endothelial progenitor cells via S1PR1/S1PR3/PI3K/Akt pathway. Cell Biol Int. 2018 Nov;42(11):1492-1502. doi: 10.1002/cbin.10991. | ||
作用机制 | CYM 5541 sits in the hydrophobic pocket close to F263[3]. |
实验方案 | |||
---|---|---|---|
1mg | 5mg | 10mg | |
1 mM 5 mM 10 mM |
3.16mL 0.63mL 0.32mL |
15.80mL 3.16mL 1.58mL |
31.60mL 6.32mL 3.16mL |
参考文献 |
---|