AM095 suppresses the LPA-triggered calcium movement in CHO cells that are genetically modified to express either human or mouse LPA1. The IC50 values for the suppression of LPA-evoked calcium movement by AM095 in CHO cells expressing human or mouse LPA1 are 0.025 μM and 0.023 μM, respectively[1]. AM095 diminishes the LPA-induced vasorelaxation by approximately 90% at a concentration of 10 μM compared to the control treated with a vehicle[2]. AM095 hinders the LPA-driven chemotaxis of CHO cells that overexpress mouse LPA1 (IC50=778 nM) and human A2058 melanoma cells (IC50=233 nM)[3].
体内研究
AM095 exhibits notable oral bioavailability and a moderate half-life, showing tolerability in rats and dogs following oral and intravenous administration. AM095 progressively inhibits the LPA-induced release of histamine. It also reduces the bleomycin-triggered rise in collagen, protein, and the infiltration of inflammatory cells in bronchoalveolar lavage fluid. Additionally, AM095 lessens kidney fibrosis in a model of unilateral ureteral obstruction in mice[3].
体外研究
AM095 suppresses the LPA-triggered calcium movement in CHO cells that are genetically modified to express either human or mouse LPA1. The IC50 values for the suppression of LPA-evoked calcium movement by AM095 in CHO cells expressing human or mouse LPA1 are 0.025 μM and 0.023 μM, respectively[1].
AM095 diminishes the LPA-induced vasorelaxation by approximately 90% at a concentration of 10 μM compared to the control treated with a vehicle[2].
AM095 hinders the LPA-driven chemotaxis of CHO cells that overexpress mouse LPA1 (IC50=778 nM) and human A2058 melanoma cells (IC50=233 nM)[3].
搜索
