Description | CYM50260 is a potent and exquisitely selective agonist of sphingosine-1-phosphate 4 receptor (S1P4-R, EC50= nM) with no activity against S1P1-R, S1P2-R, S1P3-R and S1P5-R. |
In vitro | CYM50260是一种合成的S1P4-R激动剂。它能抑制由胶原蛋白引起的血小板聚集、sCD40L释放和PDGF-AB分泌。研究发现,CYM50260的效力是首次发现的活性化合物(HTS-hit)[1]的3.5倍。此外,CYM50260还能降低胶原蛋白导致的磷酸化HSP27的释放以及HSP27的磷酸化作用[2]。 |
Target activity | S1P4 R:(EC50)45 nM |
molecular weight | 350.6 |
Molecular formula | C14H11Cl3FNO2 |
CAS | 1355026-60-6 |
Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
Solubility | DMSO: 50 mg/mL (142.61 mM) |
References | 1. Guerrero M, et al. Discovery, design and synthesis of novel potent and selective sphingosine-1-phosphate 4 receptor (S1P₄-R) agonists. Bioorg Med Chem Lett. 2012 Jan 1;22(1):537-42. 2. Onuma T, et al. Sphingosine 1-phosphate (S1P) suppresses the collagen-induced activation of human platelets via S1P4 receptor. Thromb Res. 2017 Aug;156:91-100. |