lpa3

Tetradecyl phosphonate is a pan-antagonist of lysophosphatidic acid 1 (LPA1), LPA2, and LPA3 receptors.

Ki16198 is an orally available LPA receptor antagonist and is a methyl ester derivative of Ki16425. It inhibits LPA1- and LPA3-induced inositol phosphates with Ki values of 0.34 and 0.93 μM, respectively, and can be used in studies of pancreatic carcinogenesis and metastasis.

LPA2 antagonist 2 is a selective and potent LPA2 antagonist (IC50: 28.3 nM) with potential anticancer activity, inhibits LPA3, and can be used in the study of cancer.

H2L 5765834 is a lysophosphatidic acid receptors antagonist

VPC32183 is a competitive antagonist of LPA1 and LPA3 receptors.

Ki16425 (Debio 0719) is a competitive, potent, and reversible antagonist to LPA1, LPA2, and LPA3, with Ki values of 0.34 μM, 6.5 μM, and 0.93 μM, respectively.

VPC 32183 (S) is a competitive antagonist at the LPA1 and LPA3 receptors. VPC 32183 is devoid of agonist activity at the human LPA1, LPA2 and LPA3 receptors, and, presumably, at other mammalian LPA receptors.

1-Linoleoyl lysophosphatidic acid (1-linoleoyl LPA), a glycerophospholipid with linoleic acid at its sn-1 position, acts as an LPA2 receptor agonist and is the predominant LPA form in both mouse and human plasma. This compound preferentially boosts intracellular calcium in Sf9 cells expressing the LPA2 receptor (EC50 = ~10 nM), compared to those with LPA1 and LPA3 receptors (EC50s = ~200 and ~80 nM, respectively). Notably, 1-linoleoyl LPA serum concentrations are elevated in mice with NCTC clone 2472 tumors, while its plasma levels are reduced in primary progressive multiple sclerosis patients—unlike in those with relapsing-remitting multiple sclerosis—and inversely associate with the severity of neurological deficits.

XY-4, a derivative of 1-palmitoyl lysophosphatidic acid (1-palmitoyl LPA094) and an agonist of peroxisome proliferator-activated receptor γ (PPARγ), effectively induces reporter gene expression in RAW 264.7 macrophages harboring a peroxisome proliferator-response element (PPRE) at a concentration of 5 µM. Unlike its action on PPARγ, XY-4 does not serve as an agonist for lysophosphatidic acid receptor 1 (LPA1), LPA2, or LPA3. Furthermore, at a lower concentration of 1 µM, it promotes platelet aggregation in vitro and triggers carotid artery neointima formation in rats.