lpa2

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.

LPA2 antagonist 1 is a highly efficient LPA2 antagonist.

Radioprotectin-1 is a selective agonist of LPA2 with EC50 of 25 nM for murine LPA2 GPCR and exerts radioprotective and radiomitigative action.

DBIBB is a non-lipid agonist of specific lysophosphatidic acid (LPA2) type 2 G-protein-coupled receptor. It is a potentially active molecule for the treatment of acute radiation syndrome caused by high intensity gamma rays on hematopoietic and gastrointestinal systems. It is an intermediate in organic synthesis and drug research. DBIBB can be used to prepare various compounds that reduce gastrointestinal radiation syndrome, increase intestinal crypt survival and intestinal cell proliferation, and reduce cell apoptosis.

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

GRI977143 is a selective and non-lipid agonist of LPA2 (EC50 = 3.3 μM). GRI977143 inhibits the activation of caspases 3, 7, 8, and 9 and and reduces DNA fragmentation.

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.

LPA2 antagonist 5 (EX1) functions as an antagonist of LPA2, with an IC50 value of 4.05 nM.

LPA2 antagonist 6 (example 2) acts as an antagonist of Lp(a). It inhibits the formation of Lp(a) with an IC50 value of 2.33 nM, making it useful for cardiovascular disease research.

Decyl phosphate is a selective agonist for the LPA2 receptor (EC50: 1.8 μM) and also acts as an antagonist for LPA1/LPA3 receptors. It is utilized in the research of blood disorders.

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

LPA2 antagonist 3 (compound 15) serves as an Lp(a) antagonist. Lp(a) is a pathogenic risk factor for atherosclerotic cardiovascular disease (ASCVD).

1-Arachidonoyl-2-hydroxy-sn-glycero-3-PA is a phospholipid that contains arachidonic acid at the sn-1 position, serving as a precursor to 1-Monoarachidin. It binds with the LPA2/EDG4 receptor and can inhibit the secretion of TNF-α and IL-6 induced by LPS in wild-type dendritic cells but does not affect Lpa2-/- dendritic cells. Additionally, it reduces the differentiation of HT-29 human colon cancer cells into goblet cells in the presence of sodium butyrate.

1-Arachidonoyl-2-hydroxy-sn-glycero-3-PA (sodium) [1-Arachidonoyl-sn-glycerol 3-phosphate (sodium)] is a phospholipid containing arachidonic acid at the sn-1 position. It binds to the LPA2/EDG4 receptor with an EC50 of 10 nM and is present in the rat brain, representing 37% of arachidonic acid lysophosphatidic acid species. This compound serves as a precursor to 1-arachidonoyl-sn-glycerol and inhibits the secretion of TNF-α and IL-6 from dendritic cells stimulated by wild-type LPS. Additionally, 1-arachidonoyl-2-hydroxy-sn-glycero-3-PA (sodium) can suppress the differentiation of HT-29 colon cancer cells into goblet cells in the presence of sodium butyrate.

BrP-LPA sodium is a broad-spectrum antagonist of lysophosphatidic acid (LPA), demonstrating antagonistic activity towards LPA1 (IC50 = 4520 nM), LPA2 (IC50 = 468 nM), LPA3, and LPA4. Additionally, BrP-LPA sodium exhibits partial agonistic activity at LPA5 with an EC50 of 1282 nM. It also acts as an ATX inhibitor and effectively inhibits the migration and invasion of breast cancer cells. In mouse xenograft models of breast cancer, BrP-LPA sodium induces tumor regression and anti-angiogenic effects. This compound is applicable for breast cancer research.

H2L5186303 is an LPA2 antagonist and can be used in studies about asthma treatment.

NSC-12404 is a selective non-lipid LPA2/3 agonist.

1-Arachidonoyl lysophosphatidic acid is a phospholipid containing arachidonic acid at the sn-1 position. It has been found in rat brain as 37% of the arachidonic acid-containing lysophosphatidic acid (LPA) species and is a precursor to 1-arachidonoyl glycerol . 1-Arachidonoyl lysophosphatidic acid binds to the LPA2/EDG4 receptor with an EC50 value of approximately 10 nM. It prevents TNF-α and IL-6 secretion in wild-type but not Lpa2-/- dendritic cells stimulated by LPS. It also decreases differentiation of HT-29 human colon carcinoma cells to goblet cells in the presence of sodium butyrate.

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.

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.

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.

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.