| Description | ASM-IN-1 is a potent, orally active inhibitor of acid sphingomyelinase (ASM) with an IC50 of 1.5 µM, demonstrating antiatherosclerotic and anti-inflammatory activity. It effectively reduces lipid plaques in the aortic arch and aorta, along with decreasing plasma ceramide concentrations and oxidized LDL (Ox-LDL) levels [1]. |
| In vitro | ASM-IN-1（化合物4i）不影响HUVEC细胞生长[1]。在HUVEC中，ASM-IN-1（0, 1, 5 µM）对LPS刺激的IL-6和TNF-α表达产生剂量依赖性降低作用[1]。ASM-IN-1（5 µM）减少Ox-LDL刺激的MCP-1 mRNA表达，并使IL-6 mRNA水平恢复至正常范围[1]。 |
| In vivo | ASM-IN-1（1 mg/kg 静脉注射；10 mg/kg 口服）在 ICR 小鼠中展现了优秀的药动学属性，具有 35.42% 的口服生物利用度[1]。此外，ASM-IN-1（6、12、40 mg/kg 腹腔注射，每日两次，连续 8 周）能够通过抑制 ASM 活性来有效发挥预防动脉粥样硬化的作用[1]。 |
| molecular weight | 390.19 |
| Molecular formula | C16H12BrN3O4 |
| CAS | 2913151-46-7 |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year |