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LPA Receptor Antagonist
Ki16425 is a LPA receptor antagonist with selectivity for LPA1 and LPA3 and exhibits Ki values of 0.34, 6.5, and 0.93 μM for the human LPA1, LPA2, and LPA3 receptors, respectively.- Maria F Fernandes, .et al. , Int J Mol Sci, 2022, Apr 9;23(8):4163 PMID: 35456981
- Rieko Suenaga, .et al. , PLoS One, 2022, Feb 3;17(2):e0263296 PMID: 35113924
- Inoue A, .et al. , Cell, 2019, Jun 13;177(7):1933-1947 PMID: 31160049
- Taniguchi R, .et al. , Nature, 2017, Aug 17;548(7667):356-360 PMID: 28792932
- T. HASHIMOTO, .et al. , Br J Dermatol., 2015, Nov;173(5):1334-6 PMID: 26122943
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lysophaphatidic acid 1 (LPA1/Edg-2) receptor inhibitor
SAR-100842 is a lysophaphatidic acid 1 (LPA1/Edg-2) receptor inhibitor. -
LPA1 receptor antagonist
AM966 is a high affinity, selective, oral antagonist of LPA1 receptor (lysophosphatidic acid receptor) with an IC50 value of 17 nM.- Maria F Fernandes, .et al. , Int J Mol Sci, 2022, Apr 9;23(8):4163 PMID: 35456981
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LPA1 Receptor antagonist
AM095 is a novel, potent and orally bioavailable antagonist of lysophosphatidic acid type 1 receptor (LPA1) with IC50 values of 0.73 and 0.98 μM for mouse or recombinant human LPA1, respectively -
LPA2 agonist
GRI 977143, selective lysophosphatidic acid 2 (LPA2) receptor non-lipid agonist (EC50 = 3.3 uM). -
LPA1 antagonist
ONO-7300243 is a novel, potent lysophosphatidic acid receptor 1 (LPA1) antagonist with IC50 of 0.16 μM. -
LPA2 agonist
Radioprotectin-1 is a potent and specific nonlipid agonist of lysophosphatidic acid receptor 2 (LPA2), with an EC50 value of 25 nM for murine LPA2 subtype. -
LPA1 antagonist
BMS-986020 is a high-affinity lysophosphatidic acid receptor 1 (LPA1) antagonist. -
LPA1 antagonist
LPA1 antagonist 1 is a highly selective Lysophosphatidic Acid receptor-1 (LPA1) antagonist with an IC50 of 25 nM. -
LPA2 antagonist
LPA2 antagonist 1 is a LPA2 antagonist with an IC50 of 17 nM. -
LPA1 antagonist
BMS-986020 sodium is a high-affinity lysophosphatidic acid receptor 1 (LPA1) antagonist. -
LPA Receptor Activator
1-Oleoyl lysophosphatidic acid sodium is a potent LPA receptor activator, functioning primarily as a bioactive phospholipid. This compound promotes mitosis by inducing DNA synthesis, making it critical for studies in cell proliferation. Additionally, 1-Oleoyl lysophosphatidic acid sodium plays a role in mediating both normal and pathological emotional responses, including anxiety and depression, contributing to research in neurobiology and mental health disorders. -
LPA2 Receptor Antagonist
H2L5186303 is a potent and selective antagonist of the lysophosphatidic acid receptor 2 (LPA2), exhibiting an IC50 of 9 nM. This compound induces apoptosis and effectively inhibits cell proliferation and motility. Additionally, H2L5186303 demonstrates anti-inflammatory properties, making it a valuable reagent for research involving cancer biology and inflammation pathways. -
LPAAT-β Inhibitor
CT 32228 is an inhibitor of lysophosphatidic acid acyltransferase-β (LPAAT-β), showing significant inhibition of tumor cell growth. It exhibits IC50 values in the range of 0.1-0.8 μM across various leukemia cell lines and effectively induces caspase activation in DHL-4 and Ramos cells. In combination with Rituximab, CT 32228 promotes apoptosis and demonstrates a 50% growth delay in xenograft models. This reagent is suitable for research applications targeting acute leukemia. -
LPA3 G-protein-coupled Receptor Agonist
(2S)-OMPT is a selective agonist for the LPA3 G-protein-coupled receptor, functioning as a lysophosphatidic acid analogue. This compound triggers downstream signaling pathways, including calcium influx and interleukin-6 (IL-6) release in cancer cells. Additionally, (2S)-OMPT activates critical signaling pathways such as MAPK and Akt. Its unique properties make it a valuable tool for research on ovarian cancer and other related studies. -
LPA Pan-Antagonist
BrP-LPA sodium is a pan-antagonist of lysophosphatidic acid (LPA), displaying antagonistic activity against LPA1, LPA2, LPA3, and LPA4, with IC50 values of 4520 nM and 468 nM, respectively. It also exhibits partial agonistic activity for LPA5, with an EC50 of 1282 nM, and demonstrates inhibitory effects on autotaxin (ATX). BrP-LPA sodium has been shown to effectively inhibit migration and invasion of breast cancer cells and promotes tumor regression along with anti-angiogenic effects in a mouse breast cancer xenograft model. This reagent is valuable for research focused on breast cancer mechanisms and therapeutic strategies. -
LPA Antagonist/ATX Inhibitor
BrP-LPA is a potent lysophosphatidic acid (LPA) antagonist and autotoxin (ATX) inhibitor. It exhibits broad-spectrum antagonism against LPA receptors LPA1-4, resulting in decreased blood vessel density and reduced anxiety-like behaviors. Additionally, BrP-LPA demonstrates significant anticancer activity, effectively inhibiting cell proliferation in breast, colon, and lung cancer models. This compound is valuable for research focused on cancer biology and vasculature modulation. -
LPA2 Agonist
Decyl phosphate is a selective agonist of the LPA2 receptor, exhibiting an EC50 value of 1.8 μM. Additionally, it acts as an antagonist for the LPA1 and LPA3 receptors. This compound is valuable for research applications focused on blood disorders and the modulation of lysophosphatidic acid signaling pathways. -
LPA Receptors Activator
1-Oleoyl lysophosphatidic acid is a potent activator of lysophosphatidic acid (LPA) receptors, exhibiting strong biological activity due to its high affinity for these receptors. This compound is frequently utilized in research to investigate LPA receptor signaling pathways and related cellular responses. Additionally, 1-Oleoyl lysophosphatidic acid has been shown to enhance SRE-driven β-galactosidase activity, making it a valuable tool in studies of gene expression and cellular signaling. -
LPA1 Antagonist
BMS-986278 is a potent, orally active antagonist of the lysophosphatidic acid receptor 1 (LPA1), exhibiting inhibition constants (Kbs) of 6.9 nM for human LPA1 and 4.0 nM for mouse LPA1. This compound is particularly useful for investigating pulmonary fibrotic disorders and exploring therapeutic strategies targeting LPA1 signaling pathways. Its selective activity makes it a valuable tool for elucidating the role of LPA1 in fibrotic disease mechanisms. -
LPA1 Antagonist
H2L 5765834 is a potent antagonist of lysophosphatidic acid receptors LPA1, LPA3, and LPA5, exhibiting IC50 values of 94 nM, 752 nM, and 463 nM, respectively. This compound is valuable for studies investigating the role of LPA receptors in various biological processes, including cell proliferation, migration, and survival. Its ability to selectively inhibit these receptors makes it a useful tool for research in cancer biology, fibrosis, and neurobiology. -
LPA1 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. This compound plays a significant role in modulating cellular signaling pathways associated with LPA1 activation. ONO-0740556 is valuable for research applications focused on investigating LPA1-related physiological and pathological processes, including cell proliferation, migration, and inflammatory responses. -
LPA5/GPR92 Antagonist
TC LPA5 4 is a selective antagonist of LPA5 (GPR92) with a non-lipid structure. It effectively inhibits LPA-induced aggregation of isolated human platelets, demonstrating an IC50 value of 800 nM. Additionally, TC LPA5 4 shows potent inhibition of cell proliferation and migration in thyroid cancer cells, making it a valuable tool for research in cancer biology and cell signaling pathways associated with LPA5. -
LPA1 Antagonist
ONO-9780307 is a potent antagonist of the LPA1 (lysophosphatidic acid receptor 1) with an IC50 value of 2.7 nM. This compound effectively inhibits LPA1-mediated signaling pathways, making it a valuable tool for studying the role of lysophosphatidic acid in various biological processes. It is suitable for research applications involving cellular signaling, inflammation, and cancer biology. -
LPA1 NAM
TAK-615 is a negative allosteric modulator (NAM) of the lysophosphatidic acid receptor 1 (LPA1). It exhibits high-affinity binding with a Kd of 1.7 nM, along with a lower affinity of 14.5 nM. This compound is primarily used in research focused on pulmonary fibrosis, enabling investigations into the role of LPA1 in fibrotic pathways and potential therapeutic interventions. -
LPA1 Receptor Antagonist
ACT-1016-0707 is a selective antagonist of the LPA1 receptor, demonstrating oral bioavailability. This compound is primarily utilized in research focused on fibrotic diseases, showcasing its potential to modulate pathways associated with fibrosis and related pathologies. Its specificity for the LPA1 receptor makes it a valuable tool for exploring therapeutic strategies in fibrotic conditions. -
LPAR1 Antagonist
GS-2278 is an antagonist of the lysophosphatidic acid receptor 1 (LPAR1), which plays a significant role in various signaling pathways associated with cellular proliferation and fibrosis. This compound demonstrates potential in research related to idiopathic pulmonary fibrosis (IPF), making it a valuable tool for elucidating the molecular mechanisms underlying fibrotic diseases. Its ability to modulate LPAR1 activity may provide insights into novel therapeutic strategies for IPF and similar conditions. -
LPA Receptor Agonist
NAEPA is a phosphate-mimetic derivative that functions as an agonist of lysophosphatidic acid (LPA) receptors. It is known to facilitate cellular signaling pathways associated with cell proliferation, migration, and differentiation. This compound is valuable for research applications exploring the roles of LPA in various biological processes, including cancer biology and neurobiology. -
LPA1 Antagonist
ONO-0300302 is a potent oral antagonist of the lysophosphatidic acid receptor 1 (LPA1), exhibiting an IC50 of 0.086 μM. This compound acts as a slow tight binding inhibitor, with an increasing binding affinity over time, demonstrated by a Kd of 0.34 nM at 37 °C after 2 hours. ONO-0300302 is primarily utilized in research related to benign prostatic hyperplasia (BPH). -
LPA2 Antagonist
LPA2 antagonist 2 is a selective antagonist of the lysophosphatidic acid receptor 2 (LPA2), exhibiting an IC50 of 28.3 nM and a Ki of 21.1 nM, demonstrating significant potency. This compound shows over 480-fold selectivity against LPA3, with an IC50 of 13.85 μM. LPA2 antagonist 2 is valuable for research applications involving elucidating LPA2-mediated signaling pathways and exploring its role in various biological processes. -
LPAR1 Antagonist
LPAR1 antagonist 1 is a selective antagonist of the lysophosphatidic acid receptor 1 (LPAR1) with an IC50 of 3.3 nM. This compound demonstrates significant oral bioavailability and is primarily utilized in researching pathways related to fibrosis. Its high potency and selectivity make it a valuable tool for investigating LPAR1-related biological processes and therapeutic interventions in fibrotic diseases. -
LPA5 Antagonist
LPA5 Antagonist 2 is a potent antagonist of the lysophosphatidic acid receptor 5 (LPA5). It exhibits significant efficacy in reducing nociceptive hypersensitivity, making it a valuable tool for studies focused on inflammatory and neuropathic pain mechanisms. This compound's high aqueous solubility facilitates its use in various biological assays and experimental applications. -
Anti-LPA mAb
Lpathomab is a human IgG1 monoclonal antibody (mAb) that targets lysophosphatidic acid (LPA). It effectively inhibits the release of pro-inflammatory cytokines IL-8 and IL-6 in SKOV3 cells, while also blocking LPA-induced tumor cell migration. Additionally, Lpathomab demonstrates the ability to reduce neovascularization in Matrigel plug and choroidal neovascularization (CNV) models, and it provides neuroprotection in a controlled cortical impact (CCI) mouse model. This reagent is suitable for research applications in brain injury, ovarian cancer, diabetic neuropathy, and spinal cord injury. -
LPA Receptor Activator
AzoLPA ammonium is a photoswitchable lipid that functions as an activator of the Lysophosphatidic acid receptors 1-5 (LPA1-5). This compound initiates LPA receptor signaling pathways, enabling researchers to investigate the physiological roles of LPA in various biological processes. It is particularly valuable for applications in cell signaling studies and the exploration of LPA-related mechanisms in cancer, neurobiology, and cell migration. -
LPA Receptor Modulator
N-PTyrosine PA ammonium is a lysophosphatidic acid (LPA) receptor modulator that functions primarily as a competitive inhibitor at LPA1 and a partial agonist at LPA5. This compound may inhibit LPA receptor activation and downstream signaling pathways by competing for binding sites with native agonists. Additionally, N-PTyrosine PA ammonium is capable of inducing morphological changes and promoting aggregation, as well as preventing LPA-induced morphological alterations through prior receptor desensitization. Its applications extend to the study of various conditions, including atherosclerosis and acute ischemic syndromes, such as unstable angina and myocardial infarction. -
LPA2 Antagonist
LPA2 antagonist 5 is a specific antagonist of the lysophosphatidic acid receptor 2 (LPA2), demonstrating an IC50 of 4.05 nM. This compound is valuable for research into the regulatory roles of LPA2 in various biological processes, including cancer biology and neurodegenerative diseases. Its ability to inhibit LPA2 signaling makes it an important tool for dissecting the receptor's functions and potential therapeutic targets. -
LPA5 Antagonist
LPA5 antagonist 3 functions as an antagonist of the lysophosphatidic acid receptor 5 (LPA5), exhibiting an IC50 of 170 nM. This compound is primarily utilized in research related to pain disorders and atherosclerosis, providing valuable insights into the role of LPA5 in various pathological conditions. Its effectiveness in modulating LPA5 activity makes it a significant tool for exploring therapeutic approaches in these areas. -
LPA1/LPA3 Antagonist
VPC12249 is a competitive dual antagonist of LPA1 and LPA3, exhibiting Ki values of 137 nM and 428 nM, respectively. It effectively inhibits calcium mobilization in HEK293T cells with a Ki of approximately 130 nM. This compound is useful for investigating the roles of LPA receptors in ovarian cancer and hypertensive diseases, providing valuable insights into potential therapeutic strategies. -
LPA Receptor Agonist
2ccPA sodium is a potent lysophosphatidic acid (LPA) receptor agonist. By activating LPA receptors and inhibiting the activity of the autotaxin (ATX) enzyme, it plays a significant role in regulating cell proliferation, migration, and apoptosis. This compound is valuable for research into various biological processes and disease states, including cancers, inflammation, and fibrosis. -
LPAR1 Antagonist
LPAR1 Antagonist 2 is a selective antagonist of the lysophosphatidic acid receptor 1 (LPAR1), demonstrating an average IC50 of 130 nM. This compound is utilized in research to investigate the role of LPAR1 in various physiological and pathological processes, including cancer progression and neurodegenerative diseases. Its inhibition of LPAR1 signaling makes it a valuable tool for studying receptor-mediated pathways and developing therapeutic strategies targeting this receptor. -
LPAR1 antagonist
BMT-136088 is an LPAR1 antagonist that effectively inhibits the activity of the lysophosphatidic acid receptor 1. This compound can be utilized as a positron emission tomography (PET) radioligand for the quantitative assessment of specific binding to LPA1 in lung tissues. Its application in research can enhance the understanding of LPAR1’s role in various biological processes and pathological conditions. -
LPA Inhibitor
L-NASPA ammonium is an effective LPA inhibitor that targets lysophosphatidic acid signaling pathways. It is utilized in research focused on platelet activation and related cellular processes. By inhibiting LPA, this compound aids in elucidating the mechanisms underlying platelet function and potential therapeutic interventions in related disorders. -
LPA Receptor Antagonist
LPA Receptor Antagonist-1 functions as a selective antagonist of lysophosphatidic acid (LPA) receptors, which play a crucial role in various cellular signaling pathways. This compound demonstrates significant biological activity by inhibiting LPA-mediated responses, making it a valuable tool for research into cellular processes related to cancer, fibrosis, and neurodegenerative diseases. Researchers can utilize LPA Receptor Antagonist-1 to investigate the implications of LPA signaling in multiple biological contexts. -
LPA Inhibitor
L-NASPA is a potent lysophosphatidic acid (LPA) inhibitor that plays a significant role in research related to platelet activation. By blocking LPA signaling pathways, L-NASPA enables the investigation of its effects on cellular processes involved in thrombosis and inflammation. This compound is valuable for studies aimed at understanding the physiological and pathological roles of LPA in various biological contexts.

