| Description | PCSK9-IN-11 (compound 5r) is a potent PCSK9 inhibitor with oral activity. PCSK9-IN-11 shows inhibitory activity of PCSK9 transcription in HepG2 cells (IC50= 5.7 μM). PCSK9-IN-11 can increase LDL receptor (LDLR) protein level. PCSK9-IN-11 can be used for atherosclerosis research. |
| In vitro | PCSK9-IN-11（0-25 μM，24小时）显著降低PCSK9蛋白水平，并以剂量依赖的方式增加LDLR表达[1]。 |
| In vivo | PCSK9-IN-11（0-1000 mg/kg，灌胃，一次）在体内展示出更好的安全性，其半致死剂量（LD50）值超过1000 mg/kg。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，并稍微降低血清PCSK9水平[1]。 |
| molecular weight | 381.79 |
| Molecular formula | C16H17ClFN5O3 |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year |
| Solubility | DMSO: 3.82 mg/mL (10 mM) |
| References | 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. |