S1P Receptor
The sphingosine-1-phosphate receptors are a class of G protein-coupled receptors that are targets of the lipid signalling molecule Sphingosine-1-phosphate (S1P). They are divided into five subtypes: S1PR1, S1PR2, S1PR3, S1PR4 and S1PR5. The sphingosine-1-phosphate receptors regulate fundamental biological processes such as cell proliferation, angiogenesis, migration, cytoskeleton organization, endothelial cell chemotaxis, immune cell trafficking and mitogenesis. Sphingosine-1-phosphate receptors are also involved in immune-modulation and directly involved in suppression of innate immune responses from T cells.
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Ponesimod is an orally active, selective sphingosine-1-phosphate receptor 1 (S1P1) immunomodulator.
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Siponimod is a potent and selective S1P1 receptor agonist with EC50 of 0.4 nM; >10,000 fold potency for S1P3.
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CYM 5520是选择性 S1P2 变构的激动剂(allosteric agonist)。
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CYM 5442 hydrochloride是选择性S1P1受体激动剂。
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CYM 50308是活性选择性 S1P4 激动剂。
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