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S1P Receptor Inhibitors

Cat.No. Product Name Information Product Use Citations Product Validations
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
S7180 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.
E0482 MP-A08 MP-A08 is a highly selective ATP competitive sphingosine kinase (SK) inhibitor that targets both SK1 and SK2.
E1917 SLF1081851 hydrochloride SLF1081851 hydrochloride is a potential inhibitor of Spns2 that blocks S1P release with an IC50 of 1.93 μM. It can be developed as a probe for studying Spns2 biology and immune modulation.
E1123 K145 K145 is a selective, substrate-competitive and orally active sphingosine kinase-2 (SphK2) inhibitor with an IC50 of 4.3 µM and a Ki of 6.4 µM in biochemical assays.
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.
S3412 CYM50308 CYM50308 (ML248) is a potent and selective S1P4 receptor agonist with an EC50 of 56 nM.
E4956 Ozanimod hydrochloride Ozanimod hydrochloride(Zeposia, RPC-1063 HCL) is a potent sphingosine 1-phosphate (S1P)receptor modulator and a selective agonist of S1P receptor subtypes 1 (S1P1) and 5 (S1P5) with EC50's of 1.03 nM and 8.6 nM, respectively. It can be used in the trearment of relapsing multiple sclerosis (MS).
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.
E2411 Taurodeoxycholic acid sodium hydrate Taurodeoxycholic acid sodium hydrate (Sodium taurodeoxycholate monohydrate), a bile acid, is an amphiphilic surfactant molecule synthesized from cholesterol in the liver. It activates S1PR2 pathway in addition to the TGR5 pathway.
E1218 K6PC-5 K6PC-5, a ceramide derivative, is a sphingosine kinase 1 (SPHK1) activator and elicits a rapid transient increase in intracellular calcium levels.
Cell Prolif, 2024, e13604.
Int J Biol Sci, 2022, 18(7):2994-3005
S0817 SKI-V SKI V is a noncompetitive and potent inhibitor of non-lipid sphingosine kinase with IC50 of 2 μM for GST-hSK. This compound also inhibits PI3K with IC50 of 6 μM for hPI3k. It decreases formation of the mitogenic second messenger sphingosine-1-phosphate (S1P) and induces apoptosis with antitumor activity.
Cell Death Discov, 2022, 8(1):48