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LPL Receptor Inhibitors

Cat.No. Product Name Information Product Use Citations Product Validations
S7952 Ozanimod Ozanimod is a selective oral S1P Receptor 1 modulator. Phase 3.
Nat Commun, 2025, 16(1):1826
Front Immunol, 2024, 15:1230735
FASEB J, 2022, 36(2):e22132
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
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
Verified customer review of Ki16198
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
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
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.
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).
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). This compound 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. It has the potential for the treatment of idiopathic pulmonary fibrosis (IPF).
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.