LPAR5 Antagonist

AS2717638 is a highly selective, brain-penetrant and orally active lysophosphatidic acid receptor 5 (LPA5) antagonist with an IC₅₀ value of 38 nM. AS2717638 is highly selective and shows no significant antagonistic activity against other LPA receptors (LPA1, LPA2, and LPA3). AS2717638 can be used in the research of pain and neuroinflammation-related diseases.

H2L 5765834 is an antagonist of lysophosphatidic acid receptors LPA₁, LPA₃, and LPA₅, with IC₅₀s of 94, 752, and 463 nM respectively.

BrP-LPA sodium is a pan-opposite agent for lysophosphatidic acid (LPA). It has antagonistic activity against LPA₁ (IC₅₀ = 4520 nM), LPA₂ (IC₅₀ = 468 nM), LPA₃, and LPA₄. BrP-LPA sodium also has partial agonistic activity for LPA₅, with its EC₅₀ being 1282 nM. BrP-LPA sodium has ATX inhibitory activity. BrP-LPA sodium effectively inhibits the migration and invasion of breast cancer cells. BrP-LPA sodium achieves tumor regression and anti-angiogenesis in mice breast cancer xenograft model. BrP-LPA sodium can be used for the study of breast cancer.