ML-031 is an agonist of S1P2 with EC50 value of 1 μM [1].
Sphingosine 1-phosphate (S1P) is a bioactive lysophospholipid mediator mainly released from activated platelets and implicated in many biological responses, such as cell proliferation, migration, survival, and differentiation [1]. Sphingolipids belong to a family of bioactive molecules with cell signaling properties. Sphingosine 1-phosphate (S1P) is widely expressed on various tissues and cell types. S1P is a pleiotropic lysophospholipid mediator exists in plasma and is released in large amounts from activated platelets [1]. Until now, five sphingosine-1-phosphate receptors (S1PR1-S1PR5) have been identified. S1PR4 and S1PR5 are prominently expressed in the immune and nervous systems, respectively. S1P functions by binding to five distinct G protein-coupled receptors, S1P1/EDG-1, S1P2/EDG-5, S1P3/EDG-3, S1P4/EDG-6, and S1P5/EDG-8.
ML-031 activated S1P2 with an EC50 value of 1 μM in a S1P reporter assay [1].
Reference:
[1] Satsu H, Schaeffer M T, Guerrero M, et al. A sphingosine 1-phosphate receptor 2 selective allosteric agonist[J]. Bioorganic & medicinal chemistry, 2013, 21(17): 5373-5382.