lpa1

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

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

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.

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

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.

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.

H2L 5765834 is a lysophosphatidic acid receptors antagonist

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

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

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

VPC32183 is a competitive antagonist of LPA1 and LPA3 receptors.

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.

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).

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

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.

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