| E7475 |
AM095
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AM095 is a selective LPA1 receptor antagonist. The IC50 for AM095 antagonism of LPA-induced calcium flux of human or mouse LPA1-transfected CHO cells is 0.025 and 0.023 μM, respectively.
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| E7476New |
TY-52156
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TY-52156 is an S1P3 receptor antagonist with a Ki of 110 nM.
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| S5002 |
FTY720 (Fingolimod) Hydrochloride
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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.
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Cancer Cell, 2025, S1535-6108(25)00319-8
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Nat Commun, 2025, 16(1):9175
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Nat Commun, 2025, 16(1):1826
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| S1315 |
Ki16425
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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.
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Cell Rep, 2024, 43(11):114972
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JCI Insight, 2024, 9(24)e178535
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Lipids Health Dis, 2024, 23(1):381
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| S7182 |
JTE 013
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JTE 013 is a potent and selective S1P2 antagonist with IC50 of 17.6 nM.
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Cell Death Dis, 2025, 16(1):282
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Front Pharmacol, 2024, 15:1494210
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Cell Res, 2022, 10.1038/s41422-022-00614-0
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| S2906 |
Ki16198
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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.
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Neurosci Bull, 2016, 32(5):445-54
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| S8345 |
ONO-7300243
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ONO-7300243 is a novel, potent LPA1(Lysophosphatidic Acid Receptor) antagonist with an IC50 of 160 nM.
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Eur J Pharmacol, 2020, 868:172886
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| S6633 |
AM 095
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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.
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Gastroenterology, 2022, 162(4):1210-1225
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| E2363 |
Etrasimod(APD334)
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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.
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| S3534 |
AM966
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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).
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| S3572 |
BMS-986020
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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).
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| S7181 |
W146
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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.
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