CYM-5442|CYM5442|S1P1 agonist|DC Chemicals

CYM-5442|CYM5442|S1P1 agonist|DC Chemicals
CYM-5442 is a highly-selective S1P1 (Spingosine 1-Phosphate Receptor 1) agonist.

Product name: CYM5442 |Cat No. DC8088|Other names: CYM-5442,CYM5442|Cas: 1094042-01-9|Molecule Weight: 409.48|Molecule Formular: C23H27N3O4| Purity: >98%

CYM-5442 is a highly-selective S1P1 (Spingosine 1-Phosphate Receptor 1) agonist that activates S1P1-dependent pathways in vitro and to levels of full efficacy in vivo through a hydrophobic pocket, separable from the orthosteric site of S1P binding that is headgroup dependent. This is a different site from those involved in the activities of other agonists such as FTY720 and SEW2871.CYM-5442 significantly inhibited but did not prevent aGVHD. CYM-5442 did not affect the infiltration of the donor T cells into the target organs, while the number of macrophages in GVHD organs was significantly reduced by CYM-5442 treatment. In vivo proliferation assays showed that the proliferation of macrophages was not suppressed by CYM-5442. Further studies using human endothelial cells demonstrated that CYM-5442 treatment downregulated CCL2 and CCL7 expression in endothelial cells, therefore reducing the migration of monocytes, from which tissue macrophages originate. Our data demonstrate the therapeutic efficacy of an S1P1-selective agonist in aGVHD and its possible mechanism of action. The results suggest that further investigations are needed regarding CYM-5442 as a potential therapeutic regimen for aGVHD.

For research and scientific purpose only, not for human use.