别称 | CYM5541, ML249, N,N-Dicyclohexyl(5-cyclopropylisoxazol-3-yl)-carboxamide, N,N Dicyclohexyl-5-cyclopropyl-3-isoxazolecarboxamide |
生物活性/药理作用 | CYM-5541 is an allosteric agonist selective for the Sphingosine 1-phosphate (S1P) S1P3 receptor subtype. CYM-5541 occupies a different chemical space in the ligand binding pocket of S1P3 than S1P does, a lower hydrophobic region around transmembrane helix TM6. CYM-5541 shows great selectivity and stability with an EC50 of between 72 and 132 nM compared to S1P1 EC50 > 10 μM, S1P2 EC50 > 50 μM, S1P4 EC50 > 50 μM, and S1P5 EC50 > 25 μM and no significant activities for a panel of 55 GPCRs, ion channels, and transporters. |