AM095 free acid is a potent LPA1 receptor antagonist with IC50 values of 0.98 and 0.73 μM for recombinant human or mouse LPA1 respectively.
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描述 | 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]. |
Animal study | 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]. |
计算器 | ||||
存储液制备 | ![]() |
1mg | 5mg | 10mg |
1 mM 5 mM 10 mM |
2.19mL 0.44mL 0.22mL |
10.95mL 2.19mL 1.10mL |
21.91mL 4.38mL 2.19mL |
CAS号 | 1228690-36-5 |
分子式 | C27H24N2O5 |
分子量 | 456.49 |
SMILES Code | O=C(O)CC1=CC=C(C2=CC=C(C3=C(NC(O[C@@H](C4=CC=CC=C4)C)=O)C(C)=NO3)C=C2)C=C1 |
MDL No. | MFCD22665734 |
别名 | AM095 |
运输 | 蓝冰 |
InChI Key | LNDDRUPAICPXIN-GOSISDBHSA-N |
Pubchem ID | 46213949 |
存储条件 |
In solvent -20°C:3-6个月-80°C:12个月 Pure form Inert atmosphere, room temperature |
溶解方案 |
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