| Bioactivity | PCSK9-IN-11 (compound 5r) is a potent and orally active PCSK9 inhibitor. PCSK9-IN-11 exhibits PCSK9 transcriptional inhibitory activity in HepG2 cells, with an IC50 of 5.7 μM. PCSK9-IN-11 increases LDL receptor (LDLR) protein level. PCSK9-IN-11 can be used for atherosclerosis research[1]. |
| Target | IC50: 5.7 μM (PCSK9) |
| Invitro | PCSK9-IN-11 (compound 5r) (0-25 μM, 24 h) 以剂量依赖性方式显着降低 PCSK9 蛋白水平并增加 LDLR 表达[1]。 Western Blot Analysis[1] Cell Line: |
| In Vivo | PCSK9-IN-11 (compound 5r) (0-1000 mg/kg，灌胃，once) 具有更好的体内安全特性，半致死剂量 (LD50) 值超过 1000 mg/kg [1]。PCSK9-IN-11 (30 mg/kg，灌胃，每天一次，持续 8 周) 显著抑制肝脏 PCSK9 表达并略微降低血清 PCSK9 水平[1]。 Animal Model: |
| Name | PCSK9-IN-11 |
| Formula | C16H17ClFN5O3 |
| Molar Mass | 381.79 |
| 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]. Qiao MQ, et al. Structure-activity relationship and biological evaluation of xanthine derivatives as PCSK9 inhibitors for the treatment of atherosclerosis. Eur J Med Chem. 2022 Dec 26;247:115047. |