| S5002 |
Fingolimod (FTY720) Hydrochloride
|
Fingolimod (FTY720, Fingolimod Hydrochloride) HCl is a S1P antagonist with IC50 of 0.033 nM in K562, and NK cells.Please use saline solution rather than PBS for dilutions. PBS may cause precipitation. |
-
Cancer Cell, 2025, S1535-6108(25)00319-8
-
Nat Commun, 2025, 16(1):9175
-
Nat Commun, 2025, 16(1):1826
|
|
| S7177 |
PF-543 hydrochloride
|
PF-543 hydrochloride, a novel sphingosine-competitive inhibitor of SphK1, inhibits SphK1 with IC50 and Ki of 2.0 nM and 3.6 nM, exhibits >100-fold selectivity over the SphK2 isoform. PF-543 hydrochloride induces apoptosis, necrosis, and autophagy. |
-
Cell Death Discov, 2025, 11(1):29
-
FASEB J, 2025, 39(12):e70768
-
FASEB J, 2025, 39(12):e70768
|
|
| S1315 |
Ki16425
|
Ki16425 is a competitive, potent and reversible antagonist to LPA1, LPA2 and LPA3 with Ki of 0.34 μM, 6.5 μM and 0.93 μM in RH7777 cell lines, respectively, shows no activity at LPA4, LPA5, LPA6. |
-
Cell Rep, 2024, 43(11):114972
-
JCI Insight, 2024, 9(24)e178535
-
Lipids Health Dis, 2024, 23(1):381
|
|
| S5950 |
Fingolimod (FTY-720)
|
Fingolimod (FTY-720) is a sphingosine 1-phosphate receptor modulator used for the treatment of relapsing-remitting multiple sclerosis. |
-
Nat Commun, 2024, 15(1):6970
-
Ther Adv Neurol Diso, 2024, 17:17562864241300047
-
Oncol Res, 2023, 31(6):867-875
|
|
| S7179 |
Siponimod (BAF312)
|
BAF312 (Siponimod) is a next-generation S1P receptor modulator, 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 Death Dis, 2025, 16(1):282
-
Cancers (Basel), 2024, 16(3)574
-
J Neuroinflammation, 2023, 20(1):35
|
|
| S7182 |
JTE 013
|
JTE 013 is a potent and selective S1P2 antagonist with IC50 of 17.6 nM. |
-
Cell Death Dis, 2025, 16(1):282
-
Front Pharmacol, 2024, 15:1494210
-
Cell Res, 2022, 10.1038/s41422-022-00614-0
|
|
| S7952 |
Ozanimod
|
Ozanimod is a selective oral S1P Receptor 1 modulator. Phase 3.
|
-
Nat Commun, 2025, 16(1):1826
-
Front Immunol, 2024, 15:1230735
-
Front Immunol, 2024, 15:1230735
|
|
| S8241 |
Ponesimod (ACT-128800)
|
Ponesimod (ACT-128800) is an orally active, selective sphingosine-1-phosphate receptor 1 (S1P1) immunomodulator with EC50 of 5.7 nM. |
-
Cancers (Basel), 2024, 16(3)574
-
EBioMedicine, 2023, 94:104713
-
Int J Mol Sci, 2022, 23(18)10311
|
|
| S4578 |
Tyloxapol
|
Tyloxapol (Triton WR1339) is a nonionic liquid polymer of the alkyl aryl polyether alcohol type, used as a surfactant to aid liquefaction, removal of mucopurulent and bronchopulmonary secretions. It also blocks plasma lipolytic activity, and thus the breakdown of triglyceride-rich lipoproteins.Tyloxapol can be used to induce animal models of Hyperlipidemia, Atherosclerosis. |
-
iScience, 2022, 25(10):105068
-
Front Cell Dev Biol, 2022, 10:808140
-
bioRxiv, 2020, 2020/9/20.4.7.30734
|
|
| S2906 |
Ki16198
|
Ki16198 is the methyl ester of Ki16425, which is a LPA antagonist and inhibits LPA1- and LPA3-induced inositol phosphate production with Ki of 0.34 μM and 0.93 μM, respectively, shows weaker inhibition for LPA2, no activity at LPA4, LPA5, LPA6. |
-
Neurosci Bull, 2016, 32(5):445-54
|
|
| S8345 |
ONO-7300243
|
ONO-7300243 is a novel, potent LPA1(Lysophosphatidic Acid Receptor) antagonist with an IC50 of 160 nM. |
-
Eur J Pharmacol, 2020, 868:172886
|
|
| S6633 |
AM 095
|
AM095 is an antagonist of the LPA type 1 receptor with IC50 values of 0.98 and 0.73 μM for recombinant human and mouse LPA1, respectively. |
-
Gastroenterology, 2022, 162(4):1210-1225
|
|
| S7180New |
SEW 2871
|
SEW2871 is an orally active, potent, and highly selective agonist of the sphingosine-1-phosphate type 1 receptor (S1P1) with an EC50 of 13.8 nM. It activates ERK, Akt, and Rac signalling pathways and induces S1P1 internalization and recycling. |
-
Cell Death Dis, 2021, 12(11):1050
|
|
| E2363 |
Etrasimod(APD334)
|
Etrasimod(APD334) is a potent, selective and orally available antagonist of the sphingosine-1-phosphate-1 (S1P1) receptor with an EC50 value of 1.88 nM in CHO cells. |
|
|
| S0536 |
Ibrolipim
|
Ibrolipim (NO-1886) is an effective lipoprotein lipase (LPL) activator that increases LPL mRNA and LPL activity in adipose tissue, myocardium, and skeletal muscle. |
|
|
| S3534 |
AM966
|
AM966 is a high affinity, selective, oral Lysophosphatidic acid receptor 1 (LPA1) antagonist, which can inhibit LPA-stimulated intracellular calcium release (IC50=17 nM, by Ca flux assay). |
|
|
| 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. |
-
Brain Behav Immun, 2024, 124:205-217
|
|
| E1999 |
Sphingosine-1-phosphate
|
Sphingosine-1-phosphate (S1P) is an agonist of S1P1-5 receptors and a ligand toGPR3, GPR6 and GPR12. It enhances GPR3-, GPR6-, and GPR12-mediated intracellular Ca²⁺ mobilization and regulates essential cellular processes such as proliferation, migration, cytoskeletal organization, adherens junction assembly, and morphogenesis. |
|
|
| S3572 |
BMS-986020
|
BMS-986020 (AM152, AP-3152 free acid) is a potent and selective antagonist of lysophosphatidic acid receptor 1 (LPA1). BMS-986020 inhibits bile acid and phospholipid transporters with IC50 of 4.8 μM, 6.2 μM, and 7.5 μM for BSEP, MRP4, and MDR3, respectively. BMS-986020 has the potential for the treatment of idiopathic pulmonary fibrosis (IPF). |
|
|
| E7476New |
TY-52156
|
TY - 52156は、Ki値が110 nMである強力かつ選択的なS1P3受容体拮抗薬です。 |
|
|
| 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. |
-
Front Pharmacol, 2024, 15:1494210
|
|
| S3412 |
CYM50308
|
CYM50308 (ML248) is a potent and selective S1P4 receptor agonist with an EC50 of 56 nM. |
|
|
| S7181 |
W146
|
W146 is a selective antagonist of sphingosine-1-phosphate receptor 1 (S1PR1) with an EC50 value of 398 nM. It may exhibit potential clinical applications in multiple sclerosis, coronary artery disease, diabetes, and cancer treatment. |
|
|
| A2345 |
Sonepcizumab (Anti-Sphingosine-1-phosphate)
|
Sonepcizumab (Anti-Sphingosine-1-phosphate) is a humanized monoclonal antibody directed against sphingosine 1-phosphate (S1P) with potential antiangiogenic and antineoplastic activities. MW : 145.5 KD. |
|
|
| S7179 |
Siponimod (BAF312)
|
BAF312 (Siponimod) is a next-generation S1P receptor modulator, 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 Death Dis, 2025, 16(1):282
-
Cancers (Basel), 2024, 16(3)574
-
J Neuroinflammation, 2023, 20(1):35
|
|
| S7180New |
SEW 2871
|
SEW2871 is an orally active, potent, and highly selective agonist of the sphingosine-1-phosphate type 1 receptor (S1P1) with an EC50 of 13.8 nM. It activates ERK, Akt, and Rac signalling pathways and induces S1P1 internalization and recycling. |
-
Cell Death Dis, 2021, 12(11):1050
|
|
| 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. |
-
Brain Behav Immun, 2024, 124:205-217
|
|
| E1999 |
Sphingosine-1-phosphate
|
Sphingosine-1-phosphate (S1P) is an agonist of S1P1-5 receptors and a ligand toGPR3, GPR6 and GPR12. It enhances GPR3-, GPR6-, and GPR12-mediated intracellular Ca²⁺ mobilization and regulates essential cellular processes such as proliferation, migration, cytoskeletal organization, adherens junction assembly, and morphogenesis. |
|
|
| 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. |
-
Front Pharmacol, 2024, 15:1494210
|
|
| S3412 |
CYM50308
|
CYM50308 (ML248) is a potent and selective S1P4 receptor agonist with an EC50 of 56 nM. |
|
|
| S5002 |
Fingolimod (FTY720) Hydrochloride
|
Fingolimod (FTY720, Fingolimod Hydrochloride) HCl is a S1P antagonist with IC50 of 0.033 nM in K562, and NK cells.Please use saline solution rather than PBS for dilutions. PBS may cause precipitation. |
- Cancer Cell, 2025, S1535-6108(25)00319-8
- Nat Commun, 2025, 16(1):9175
- Nat Commun, 2025, 16(1):1826
|
|
| S1315 |
Ki16425
|
Ki16425 is a competitive, potent and reversible antagonist to LPA1, LPA2 and LPA3 with Ki of 0.34 μM, 6.5 μM and 0.93 μM in RH7777 cell lines, respectively, shows no activity at LPA4, LPA5, LPA6. |
- Cell Rep, 2024, 43(11):114972
- JCI Insight, 2024, 9(24)e178535
- Lipids Health Dis, 2024, 23(1):381
|
|
| S7182 |
JTE 013
|
JTE 013 is a potent and selective S1P2 antagonist with IC50 of 17.6 nM. |
- Cell Death Dis, 2025, 16(1):282
- Front Pharmacol, 2024, 15:1494210
- Cell Res, 2022, 10.1038/s41422-022-00614-0
|
|
| S2906 |
Ki16198
|
Ki16198 is the methyl ester of Ki16425, which is a LPA antagonist and inhibits LPA1- and LPA3-induced inositol phosphate production with Ki of 0.34 μM and 0.93 μM, respectively, shows weaker inhibition for LPA2, no activity at LPA4, LPA5, LPA6. |
- Neurosci Bull, 2016, 32(5):445-54
|
|
| S8345 |
ONO-7300243
|
ONO-7300243 is a novel, potent LPA1(Lysophosphatidic Acid Receptor) antagonist with an IC50 of 160 nM. |
- Eur J Pharmacol, 2020, 868:172886
|
|
| S6633 |
AM 095
|
AM095 is an antagonist of the LPA type 1 receptor with IC50 values of 0.98 and 0.73 μM for recombinant human and mouse LPA1, respectively. |
- Gastroenterology, 2022, 162(4):1210-1225
|
|
| E2363 |
Etrasimod(APD334)
|
Etrasimod(APD334) is a potent, selective and orally available antagonist of the sphingosine-1-phosphate-1 (S1P1) receptor with an EC50 value of 1.88 nM in CHO cells. |
|
|
| S3534 |
AM966
|
AM966 is a high affinity, selective, oral Lysophosphatidic acid receptor 1 (LPA1) antagonist, which can inhibit LPA-stimulated intracellular calcium release (IC50=17 nM, by Ca flux assay). |
|
|
| S3572 |
BMS-986020
|
BMS-986020 (AM152, AP-3152 free acid) is a potent and selective antagonist of lysophosphatidic acid receptor 1 (LPA1). BMS-986020 inhibits bile acid and phospholipid transporters with IC50 of 4.8 μM, 6.2 μM, and 7.5 μM for BSEP, MRP4, and MDR3, respectively. BMS-986020 has the potential for the treatment of idiopathic pulmonary fibrosis (IPF). |
|
|
| E7476New |
TY-52156
|
TY - 52156は、Ki値が110 nMである強力かつ選択的なS1P3受容体拮抗薬です。 |
|
|
| S7181 |
W146
|
W146 is a selective antagonist of sphingosine-1-phosphate receptor 1 (S1PR1) with an EC50 value of 398 nM. It may exhibit potential clinical applications in multiple sclerosis, coronary artery disease, diabetes, and cancer treatment. |
|
|
| S7179 |
Siponimod (BAF312)
|
BAF312 (Siponimod) is a next-generation S1P receptor modulator, 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 Death Dis, 2025, 16(1):282
- Cancers (Basel), 2024, 16(3)574
- J Neuroinflammation, 2023, 20(1):35
|
|
| S7180New |
SEW 2871
|
SEW2871 is an orally active, potent, and highly selective agonist of the sphingosine-1-phosphate type 1 receptor (S1P1) with an EC50 of 13.8 nM. It activates ERK, Akt, and Rac signalling pathways and induces S1P1 internalization and recycling. |
- Cell Death Dis, 2021, 12(11):1050
|
|
| 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. |
- Brain Behav Immun, 2024, 124:205-217
|
|
| E1999 |
Sphingosine-1-phosphate
|
Sphingosine-1-phosphate (S1P) is an agonist of S1P1-5 receptors and a ligand toGPR3, GPR6 and GPR12. It enhances GPR3-, GPR6-, and GPR12-mediated intracellular Ca²⁺ mobilization and regulates essential cellular processes such as proliferation, migration, cytoskeletal organization, adherens junction assembly, and morphogenesis. |
|
|
| 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. |
- Front Pharmacol, 2024, 15:1494210
|
|
| S3412 |
CYM50308
|
CYM50308 (ML248) is a potent and selective S1P4 receptor agonist with an EC50 of 56 nM. |
|
|