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.

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

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.

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

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.

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

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

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.

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.

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

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

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.

ACT-1016-0707 is a potent, selective, and insurmountable lysophosphatidic acid receptor 1 (LPA1) antagonist,ACT-1016-0707 demonstrates pronounced antifibrotic and anti-inflammatory activities in experimental models. ACT-1016-0707 has been studied extensively in vitro and in vivo lung fibrosis models, where it reduces pathological fibrotic progression, thereby representing a candidate compound for research into fibrotic lung diseases.

H2L 5765834 is a lysophosphatidic acid receptors antagonist

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

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

HL001 is an orally active small molecule inhibitor of cyclophilin A (CypA) and a receptor antagonist of lysophosphatidic acid 1 (LPA1). It induces cell cycle arrest and apoptosis in tumor cells via p53. By downregulating G3BP1, HL001 promotes reactive oxygen species production and DNA damage to stabilize p53. It disrupts the interaction between MDM2 and p53-72R in a CypA-dependent manner. HL001 exhibits antitumor activity and can also be used in research on pulmonary fibrosis.

UCM-05194 (ammonium) is an agonist for the lysophosphatidic acid receptor 1 (LPA1). It induces calcium mobilization in RH7777 cells expressing LPA1, with an EC50 of 0.24 µM. In B103 rat neuroblastoma cells that overexpress LPA1, UCM-05194 (ammonium) promotes neurite retraction and cell migration. Additionally, it alleviates acetic acid-induced writhing and mechanical hyperalgesia in mice.

AzoLPA ammonium is a photoswitchable lipid that activates signaling of lysophosphatidic acid receptors 1-5 (LPA1-5).

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.

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.

BrP-LPA is an LPA antagonist and ATX inhibitor, exhibiting broad-spectrum antagonistic activity against LPA1-4 GPCR. It effectively reduces vascular density and dose-dependently inhibits Lysophosphatidic acid-induced head-dipping behavior. BrP-LPA also demonstrates anticancer properties against breast, colon, and lung cancer while additionally inhibiting anxiety-like behavior.