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S1P Receptor

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S1P Receptor Products

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  • S1P Receptor Inhibitors (2)
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  • S1P Receptor Antagonists (2)
  • S1P Receptor Agonists (4)
  • S1P Receptor Modulators (5)
  • New S1P Receptor Products
Catalog No. Product Name Information Product Use Citations Product Validations
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.
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).
Elife, 2021, 10e63810
Breast Cancer Res, 2021, 23(1):107
Cell Death Discov, 2021, 7(1):223
S5002 Fingolimod (FTY720) HCl Fingolimod (FTY720) HCl is a S1P antagonist with IC50 of 0.033 nM in K562, and NK cells.
Nature, 2021, 10.1038/s41586-021-04044-7
Immunity, 2021, 54(10):2273-2287.e6
Mol Oncol, 2021, 10.1002/1878-0261.12970
S7182 JTE 013 JTE 013 is a potent and selective S1P2 antagonist with IC50 of 17.6 nM.
Vascul Pharmacol, 2021, S1537-1891(21)00113-0
Elife, 2020, 9e60541
Cancer Manag Res, 2020, 12:7857-7865
S3412 CYM50308 CYM50308 (ML248) is a potent and selective S1P4 receptor agonist with an EC50 of 56 nM.
S4462New 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.
J Nanobiotechnology, 2021, 19(1):165
Front Immunol, 2020, 8;11:635
Antiviral Res, 2020, S0166-3542(20)30413-7
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.
Cell, 2021, 184(19):4981-4995.e14
Phytother Res, 2021, 10.1002/ptr.7211
Front Immunol, 2020, 11:559382
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.
China Biotechnology, 2020, (6): 10-19
Nucleic Acids Res, 2019, 10.1093/nar/gkz1136
Leukemia, 2019, 10.1038/s41375-019-0478-9
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.
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).
Elife, 2021, 10e63810
Breast Cancer Res, 2021, 23(1):107
Cell Death Discov, 2021, 7(1):223
S5002 Fingolimod (FTY720) HCl Fingolimod (FTY720) HCl is a S1P antagonist with IC50 of 0.033 nM in K562, and NK cells.
Nature, 2021, 10.1038/s41586-021-04044-7
Immunity, 2021, 54(10):2273-2287.e6
Mol Oncol, 2021, 10.1002/1878-0261.12970
S7182 JTE 013 JTE 013 is a potent and selective S1P2 antagonist with IC50 of 17.6 nM.
Vascul Pharmacol, 2021, S1537-1891(21)00113-0
Elife, 2020, 9e60541
Cancer Manag Res, 2020, 12:7857-7865
S3412 CYM50308 CYM50308 (ML248) is a potent and selective S1P4 receptor agonist with an EC50 of 56 nM.
S4462New 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.
J Nanobiotechnology, 2021, 19(1):165
Front Immunol, 2020, 8;11:635
Antiviral Res, 2020, S0166-3542(20)30413-7
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.
Cell, 2021, 184(19):4981-4995.e14
Phytother Res, 2021, 10.1002/ptr.7211
Front Immunol, 2020, 11:559382
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.
China Biotechnology, 2020, (6): 10-19
Nucleic Acids Res, 2019, 10.1093/nar/gkz1136
Leukemia, 2019, 10.1038/s41375-019-0478-9
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
S4462New 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.