| Bioactivity | ASM-IN-1 is a potent and orally active acid sphingomyelinase (ASM) inhibitor with an IC50 value of 1.5 µM. ASM-IN-1 reduces lipid plaques in the aortic arch and aorta and reduces plasma ceramide concentration and Ox-LDL levels. ASM-IN-1 shows antiatherosclerotic and anti-inflammatory activity[1]. |
| Invitro | ASM-IN-1 (compound 4i) 不影响 HUVEC 中的细胞生长[1]。ASM-IN-1 (0, 1, 5 µM) 以剂量依赖的方式降低 HUVEC 中 LPS 刺激的 IL-6 和 TNF-α 的表达刺激[1] 。ASM-IN-1 (5 µM) 降低 Ox-LDL 刺激的 MCP-1 mRNA 表达并将 IL-6 mRNA 恢复到正常水平[1]。 Cell Cytotoxicity Assay[1] Cell Line: |
| In Vivo | ASM-IN-1 (1 mg/kg 静脉注射；10 mg/kg 口服) 在 ICR 小鼠中表现出良好的药代动力学特性，口服生物利用度为 35.42%[1]。ASM-IN-1 (6、12、40 mg/kg；腹腔注射；每天两次，持续 8 周) 通过抑制 ASM 在小鼠体内发挥抗动脉粥样硬化活性[1]。 |
| Name | ASM-IN-1 |
| Formula | C16H12BrN3O4 |
| Molar Mass | 390.19 |
| Transport | Room temperature in continental US; may vary elsewhere. |
| Storage | Please store the product under the recommended conditions in the Certificate of Analysis. |
| Reference | [1]. Yang K, et al. Discovery of Novel N-Hydroxy-1,2,4-oxadiazole-5-formamides as ASM Direct Inhibitors for the Treatment of Atherosclerosis. J Med Chem. 2023 Feb 23;66(4):2681-2698. |