lpa1

LPA1 receptor antagonist 1(LPA1 R antagonist 1) is a selective and potent lysophosphatidic acid (LPA1) receptor antagonist (IC50 : 25 nM) for the study of idiopathic pulmonary fibrosis.

ACT-1016-0707 (Compound 49), a selective antagonist of the LPA1 receptor, is effective when administered orally. It is utilized in the study of fibrotic diseases [1].

LPA receptor antagonist-1 (example 52) serves as an antagonist for the lysophosphatidic acid (LPA) receptor and is applicable in various types of studies [1].

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

UCM-05194 is a selective LPA1 receptor agonist that can improve neuropathic pain and can be used in the study of progressive system diseases.

1-Oleoyl lysophosphatidic acid sodium (1-Oleoyl lysophosphatidic acid sodium salt) salt is an Endogenous agonist of LPA1 and LPA2

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.

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.

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.

AM966, a excellent affinity, specific, oral LPA1(IC50=17 nM) antagonist, suppresses LPA-stimulated intracellular calcium release.

BMS-986020 (AM152) is a selective LPA1 antagonist.

TAK-615 is commonly used to study pulmonary fibrosis and is a negative allosteric modulator of LPA1 receptors.

ONO-0300302 is a slow tight binding LPA1 antagonist (IC50: 0.16 nM) used to treat Benign Prostatic Hyperplasia. ONO-0300302 inhibits significantly an LPA-induced increase of intraurethral pressure (IUP) in rat (3 mg/kg, p.o.) and dog (1 mg/kg, p.o.) over

ONO-7300243 is an antagonist of lysophosphatidic acid receptor 1 (LPA1; IC50 : 0.16 µM).

ONO-9780307 is a specific antagonist of LPA1 (lysophosphatidic acid receptor 1) (IC50: 2.7 nM).

BMS-986020 sodium is a high-affinity lysophosphatidic acid receptor 1 (LPA1) antagonist that inhibits bile acids and phospholipid transport proteins, and inhibits BSEP (IC50: 4.8 μM), MRP4 (IC50: 6.2 μM) and MDR3 (IC50: 7.5 μM). BMS-986020 sodium showed potential for the study of idiopathic pulmonary fibrosis (IPF).

H2L 5765834 is a lysophosphatidic acid receptors antagonist

Oleoyl-L-alpha-lysophosphatidic acid sodium salt is an essential cell membrane biosynthetic metabolite that mediates signal transduction by interacting with G protein-coupled receptors (GPCRs) (ie, LPA receptors). It is the receptor of LPA1 and LPA2. endogenous agonist.

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

VPC32183 is a competitive antagonist of LPA1 and LPA3 receptors.

NAEPA, an LPA mimetic, is a selective agonist of the lysophosphatidic acid-1 (LPA1) receptor.

VPC12249, a lysophosphatidic acid receptor type 1 (LPA1) antagonist, plays a functional role in osteoclast differentiation and bone resorption activity.

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

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.

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.

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.

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.

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.