| 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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| 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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| E1036 |
BMS-986278
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BMS-986278 is a potent and orally active antagonist of lysophosphatidic acid receptor 1 (LPA1). This compound exhibits Kbs of 6.9 nM and 4.0 nM for human and mouse LPA1, respectively, and is widely used in the research of pulmonary fibrotic diseases.
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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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| E1941 |
ACT-1016-0707
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ACT-1016-0707 (LPA1 receptor antagonist 2) is an orally active and selective antagonist of LPA1 Receptor, with IC50 of 3.1 nM for hLPAR1 in tango assay. It has the potential to treat fibrotic diseases.
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| E2992 |
Oleoyl-L-alpha-lysophosphatidic acid sodium salt
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Oleoyl-L-alpha-lysophosphatidic acid sodium salt is an essential metabolite for membrane biosynthesis. LPA interacts with the G protein-coupled receptors (GPCRs), called the LPA receptor and mediates signaling. It acts as a endogenous agonist for LPA1 and LPA2 receptors.
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