human lpa1

BMS-986278 is an orally active and potent hemophosphatidic acid receptor 1 (LPA1) antagonist with Kb values of 6.9 nM and 4.0 nM for human and mouse LPA1, respectively.BMS-986278 may be investigated for use in idiopathic pulmonary fibrosis.

AM095 (free acid) is a potent LPA1 receptor antagonist with IC50 values of 0.98 μM for recombinant human LPA1 and 0.73 μM for recombinant mouse LPA1.

ASP6432 is an antagonist of type 1 lysophosphatidic acid receptor (LPA1). For human LPA1 and rat LPA1, the IC50s are 11 nM and 30 nM , respectively.

AM095 is a potent LPA1 receptor antagonist with IC50 values of 0.98 and 0.73 μM for recombinant human or mouse LPA1 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.

ONO-0740556 is a potent agonist of the Gi-coupled human lysophosphatidic acid receptor 1 (LPA1), exhibiting an EC50 value of 0.26 nM.

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.

1-Arachidoyl lysophosphatidic acid (1-arachidoyl LPA), a glycerophospholipid with arachidic acid at the sn-1 position, functions as an agonist for lysophosphatidic acid receptor 1 (LPA1). It effectively induces calcium mobilization in primary human lung fibroblasts at an EC50 value of 3.6 µM, given these cells inherently express LPA1 but lack expression of LPA2-LPA6 receptors. Additionally, at a concentration of 2.5 µM, 1-arachidoyl LPA binds to the ligand-binding domain of peroxisome proliferator-activated receptor γ (PPARγ) in a cell-free environment. This compound has also been detected in human urine.