CYM-5541

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Chemical Structure| 945128-26-7 同义名 : ML249; CID-17253208
CAS号 : 945128-26-7
货号 : A108628
分子式 : C19H28N2O2
纯度 : 99%+
分子量 : 316.44
MDL号 : MFCD09782785
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 : -
动物实验配方:
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

[1]Jo E, Bhhatarai B, et al. Novel selective allosteric and bitopic ligands for the S1P(3) receptor. ACS Chem Biol. 2012 Dec 21;7(12):1975-83.

[2]Guerrero M, Poddutoori R, et al. Probe Development Efforts for an Allosteric Agonist of the Sphingosine 1-phosphate Receptor 3 (S1P3). 2011 Aug 31 [updated 2013 Feb 25] . Probe Reports from the NIH Molecular Libraries Program [Internet] .

[3]Jo E, Bhhatarai B, Repetto E, et al. Novel selective allosteric and bitopic ligands for the S1P(3) receptor. ACS Chem Biol. 2012 Dec 21;7(12):1975-83