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S1P Receptor

Choose Selective S1P Receptor Inhibitors

S1P Receptor Signaling Pathway Map

Isoform-selective Inhibitors

S1P Receptor Products

All (15)
S1P Receptor Inhibitors (2)
S1P Receptor Activator (1)
S1P Receptor Antagonists (3)
S1P Receptor Agonists (4)
S1P Receptor Modulators (5)
New S1P Receptor Products

Catalog No.	Product Name	Information	Product Use Citations
S0817	SKI-V	SKI V is a noncompetitive and potent inhibitor of non-lipid sphingosine kinase with IC50 of 2 μM for GST-hSK. SKI-V also inhibits PI3K with IC50 of 6 μM for hPI3k. SKI-V decreases formation of the mitogenic second messenger sphingosine-1-phosphate (S1P) and induces apoptosis with antitumor activity.	Cell Death Discov, 2022, 8(1):48
S6418	PF 429242	PF 429242 is known as a S1P inhibitor with an IC50 of 170 nM, showing no significant inhibition of trypsin, elastase, proteinase K, plasmin, kallikren, factor XIa, thrombin, or furin at concentrations up to 100 μM and only modest inhibition of urokinase (IC50 = 50 μM) and factor Xa (IC50 = 100 μM).	Nat Commun, 2019, 11;10(1):4621
S7791	Phorbol 12-myristate 13-acetate (PMA)	Phorbol 12-myristate 13-acetate (PMA,12-O-Tetradecanoylphorbol-13-acetate, TPA, Phorbol myristate acetate), a potent activator of PKC, is active at nanomolar concentrations. Phorbol 12-myristate 13-acetate (PMA) induces sphingosine-1-phosphate (S1P).	Cell Mol Immunol, 2022, 10.1038/s41423-022-00841-w Oncogene, 2022, 10.1038/s41388-022-02197-x Sci Rep, 2022, 12(1):1626
E2363^New	APD334	APD334 (Etrasimod ) is a potent, selective and orally available antagonist of the sphingosine-1-phosphate-1 (S1P1) receptor with an IC₅₀ value of 1.88 nM in CHO cells.
S5002	Fingolimod (FTY720) HCl	Fingolimod (FTY720) HCl is a S1P antagonist with IC50 of 0.033 nM in K562, and NK cells.	Cancer Cell, 2022, S1535-6108(22)00004-6 J Clin Invest, 2022, 132(3)e153604 J Immunother Cancer, 2022, 10(5)e003960
S7182	JTE 013	JTE 013 is a potent and selective S1P2 antagonist with IC50 of 17.6 nM.	Cell Res, 2022, 10.1038/s41422-022-00614-0 Autophagy, 2022, 1-20 Vascul Pharmacol, 2021, S1537-1891(21)00113-0
S3412	CYM50308	CYM50308 (ML248) is a potent and selective S1P4 receptor agonist with an EC50 of 56 nM.
S4462	CYM-5520	CYM-5520 is a highly selective sphingosine-1-phosphate receptor 2 (S1PR2) agonist with an EC50 of 0.48 µM and does not activate other S1P receptors.
S6552	CYM5541	CYM5541 (ML249) is a selective, allosteric agonist of S1P3 with an EC50 of between 72 and 132 nM and exhibits exquisite selectivity over other S1P receptor subtypes in vitro: S1P1 EC50 > 10 μM, S1P2 EC50 > 50 μM, S1P4 EC50 > 50 μM, and S1P5 EC50 > 25 μM.
S7179	Siponimod (BAF312)	BAF312 (Siponimod) is a next-generation S1P receptor agonist, selective for S1P1 and S1P5 receptors with EC50 of 0.39 nM and 0.98 nM, exhibits >1000-fold selectivity over S1P2, S1P3 and S1P4 receptors. Phase 3.	Cell Res, 2022, 10.1038/s41422-022-00614-0 FASEB J, 2022, 36(2):e22132 J Nanobiotechnology, 2021, 19(1):165
S2878	CYM-5442	CYM-5442 is a potent and selective S1P₁ agonist with EC50 of 1.35 nM.	Antiviral Res, 2020, S0166-3542(20)30413-7
S5950	Fingolimod	Fingolimod (FTY-720A, FTY-720) is a sphingosine 1-phosphate receptor modulator used for the treatment of relapsing-remitting multiple sclerosis.	J Clin Invest, 2022, 132(3)e153604 J Immunother Cancer, 2022, 10(5)e003960 Clin Transl Med, 2022, 12(2):e695
S7180	SEW 2871	SEW 2871 is a highly selective, orally active S1P1 agonist with EC50 of 13.8 nM.	Cell Death Dis, 2021, 12(11):1050
S7952	Ozanimod (RPC1063)	Ozanimod (RPC1063) is a selective oral S1P Receptor 1 modulator. Phase 3.	FASEB J, 2022, 36(2):e22132 China Biotechnology, 2020, (6): 10-19 Nucleic Acids Res, 2019, 10.1093/nar/gkz1136
S8241	Ponesimod	Ponesimod (ACT-128800) is an orally active, selective sphingosine-1-phosphate receptor 1 (S1P1) immunomodulator with EC50 of 5.7 nM.	Antiviral Res, 2020, S0166-3542(20)30413-7 FEBS Open Bio, 2020, 10.1002/2211-5463.12951 Leukemia, 2019, 10.1038/s41375-019-0478-9
S0817	SKI-V	SKI V is a noncompetitive and potent inhibitor of non-lipid sphingosine kinase with IC50 of 2 μM for GST-hSK. SKI-V also inhibits PI3K with IC50 of 6 μM for hPI3k. SKI-V decreases formation of the mitogenic second messenger sphingosine-1-phosphate (S1P) and induces apoptosis with antitumor activity.	Cell Death Discov, 2022, 8(1):48
S6418	PF 429242	PF 429242 is known as a S1P inhibitor with an IC50 of 170 nM, showing no significant inhibition of trypsin, elastase, proteinase K, plasmin, kallikren, factor XIa, thrombin, or furin at concentrations up to 100 μM and only modest inhibition of urokinase (IC50 = 50 μM) and factor Xa (IC50 = 100 μM).	Nat Commun, 2019, 11;10(1):4621
S7791	Phorbol 12-myristate 13-acetate (PMA)	Phorbol 12-myristate 13-acetate (PMA,12-O-Tetradecanoylphorbol-13-acetate, TPA, Phorbol myristate acetate), a potent activator of PKC, is active at nanomolar concentrations. Phorbol 12-myristate 13-acetate (PMA) induces sphingosine-1-phosphate (S1P).	Cell Mol Immunol, 2022, 10.1038/s41423-022-00841-w Oncogene, 2022, 10.1038/s41388-022-02197-x Sci Rep, 2022, 12(1):1626
E2363^New	APD334	APD334 (Etrasimod ) is a potent, selective and orally available antagonist of the sphingosine-1-phosphate-1 (S1P1) receptor with an IC₅₀ value of 1.88 nM in CHO cells.
S5002	Fingolimod (FTY720) HCl	Fingolimod (FTY720) HCl is a S1P antagonist with IC50 of 0.033 nM in K562, and NK cells.	Cancer Cell, 2022, S1535-6108(22)00004-6 J Clin Invest, 2022, 132(3)e153604 J Immunother Cancer, 2022, 10(5)e003960
S7182	JTE 013	JTE 013 is a potent and selective S1P2 antagonist with IC50 of 17.6 nM.	Cell Res, 2022, 10.1038/s41422-022-00614-0 Autophagy, 2022, 1-20 Vascul Pharmacol, 2021, S1537-1891(21)00113-0
S3412	CYM50308	CYM50308 (ML248) is a potent and selective S1P4 receptor agonist with an EC50 of 56 nM.
S4462	CYM-5520	CYM-5520 is a highly selective sphingosine-1-phosphate receptor 2 (S1PR2) agonist with an EC50 of 0.48 µM and does not activate other S1P receptors.
S6552	CYM5541	CYM5541 (ML249) is a selective, allosteric agonist of S1P3 with an EC50 of between 72 and 132 nM and exhibits exquisite selectivity over other S1P receptor subtypes in vitro: S1P1 EC50 > 10 μM, S1P2 EC50 > 50 μM, S1P4 EC50 > 50 μM, and S1P5 EC50 > 25 μM.
S7179	Siponimod (BAF312)	BAF312 (Siponimod) is a next-generation S1P receptor agonist, selective for S1P1 and S1P5 receptors with EC50 of 0.39 nM and 0.98 nM, exhibits >1000-fold selectivity over S1P2, S1P3 and S1P4 receptors. Phase 3.	Cell Res, 2022, 10.1038/s41422-022-00614-0 FASEB J, 2022, 36(2):e22132 J Nanobiotechnology, 2021, 19(1):165
S2878	CYM-5442	CYM-5442 is a potent and selective S1P₁ agonist with EC50 of 1.35 nM.	Antiviral Res, 2020, S0166-3542(20)30413-7
S5950	Fingolimod	Fingolimod (FTY-720A, FTY-720) is a sphingosine 1-phosphate receptor modulator used for the treatment of relapsing-remitting multiple sclerosis.	J Clin Invest, 2022, 132(3)e153604 J Immunother Cancer, 2022, 10(5)e003960 Clin Transl Med, 2022, 12(2):e695
S7180	SEW 2871	SEW 2871 is a highly selective, orally active S1P1 agonist with EC50 of 13.8 nM.	Cell Death Dis, 2021, 12(11):1050
S7952	Ozanimod (RPC1063)	Ozanimod (RPC1063) is a selective oral S1P Receptor 1 modulator. Phase 3.	FASEB J, 2022, 36(2):e22132 China Biotechnology, 2020, (6): 10-19 Nucleic Acids Res, 2019, 10.1093/nar/gkz1136
S8241	Ponesimod	Ponesimod (ACT-128800) is an orally active, selective sphingosine-1-phosphate receptor 1 (S1P1) immunomodulator with EC50 of 5.7 nM.	Antiviral Res, 2020, S0166-3542(20)30413-7 FEBS Open Bio, 2020, 10.1002/2211-5463.12951 Leukemia, 2019, 10.1038/s41375-019-0478-9
E2363^New	APD334	APD334 (Etrasimod ) is a potent, selective and orally available antagonist of the sphingosine-1-phosphate-1 (S1P1) receptor with an IC₅₀ value of 1.88 nM in CHO cells.