LPAR3 Antagonist

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.

BrP-LPA is a LPA antagonist/ATX inhibitor. BrP-LPA shows pan-antagonist activity towards LPA_1-4 GPCRs. BrP-LPA decreases blood vessel density. BrP-LPA dose-dependently inhibits Lysophosphatidic acid-induced head-dip counts. BrP-LPA exhibits anticancer activity against breast cancer, colon cancer, and lung cancer. BrP-LPA inhibits anxiety-like behavior.