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. 2016 Apr 28;173(11):1778–1792. doi: 10.1111/bph.13476

Figure 2.

Figure 2

RPC1063 is a potent S1P1 receptor (S1P1R) agonist and induces sustained receptor internalization. (A) S1P1 receptor CREbla CHO‐K1 cells were incubated with 2 μM forskolin in the presence of increasing doses of compound for 4 h. Inhibition of forskolin‐induced cAMP generation is indicative of agonist activity on Gi/o coupled S1P1 receptors. (B) Representative histograms of transfected HEK293T cells expressing S1P1 receptors incubated with vehicle control or 1 μM RPC1063. HEK293T cells were incubated with increasing doses of compound for 1 h (C), or for 1 h followed by extensive washing to remove compound, then a 24 h recovery period (D) and cell surface receptor expression was monitored. Error bars represent SEM of triplicate assays.