S1P (1 μM) induces a significant Ca releases in HEK293 cells under serum starvation conditions (1% FCS).
In a functional Ca assay, Suramin (HY-B0879) alone does not exert any effect on intracellular Ca release via gpr3, gpr6 or gpr12. In contrast, S1P (1 μM) induces Ca release of gpr3, gpr6 and gpr12 in the presence of Suramin (HY-B0879) various concentrations in transfected HEK293 cells.
In a functional Ca assay,S1P (3-3000 nM) in the presence Suramin (300 μM), exhibits nanomolar EC50 values for gpr3 (EC50=29 nM), gpr6 (EC50=15 nM) and gpr12 (EC50=24 nM), rat gpr3 (EC50=68 nM),respectively in HEK293 cells.
S1P increases intracellular calcium levels in TAg-Jurkat cells expressing S1P1 and Gqi5, which allows for phospholipase C stimulation by Gi proteins, when used at a concentration of 200 nM, as well as in TAg-Jurkat cells expressing S1P2 and S1P3 receptors (EC50s = 8 and 11 nM, respectively).
Medlife has not independently confirmed the accuracy of these methods. They are for reference only.