lpa5

TC LPA5 4 is a LPA5 receptor antagonist.

LPA5 antagonist 2 is a highly water-soluble, selective antagonist of the lysosomal phosphatidic acid receptor 5 (LPA5) that inhibits downstream calcium mobilization (IC₅₀ = 69 nM) and cAMP signaling (IC₅₀ = 340 nM) by blocking the binding of its natural ligand, LPA. LPA5 antagonist 2 significantly alleviates CFA-induced inflammatory pain and nociceptive hypersensitivity and can be used in research related to inflammatory and neuropathic pain.

LPA5 antagonist 1 is a highly potent and selective antagonist of lysophosphatidic acid receptor 5 (LPA5), with an IC₅₀ value of 32 nM. LPA5 antagonist 1 is a small molecule with high brain permeability that significantly alleviates mechanical allodynia in a CFA-induced inflammatory pain model and can be used to study the mechanisms underlying inflammatory and neuropathic pain. LPA5 antagonist 1 is a click chemistry reagent containing an alkyne functional group, capable of undergoing a copper-catalyzed azide-alkyne cycloaddition (CuAAC) reaction with molecules bearing an azide group.

LPA5 antagonist 3 (Example 74), a lysophosphatidic acid receptor 5 (LPA5) antagonist, exhibits potent activity with an IC50 value of 170 nM. It is primarily utilized in the research of pain disorders and atherosclerosis [1].

AS2717638 is an orally active and selective lysophosphatidic acid receptor 5 (LPA5) antagonist (IC50: 38 nM for hLPA5). It also significantly improves PGF2α-, PGE2-, and AMPA-induced allodynia.

H2L 5765834 is a lysophosphatidic acid receptors antagonist

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.