PCSK9-IN-10是一种有效的口服 PCSK9 抑制剂,IC50 值为 6.4 μM,可增加 LDLR 蛋白表达并降低 PCSK9 表达,减缓动脉粥样硬化进展,可用于高脂血症研究。
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描述 | PCSK9-IN-10 is a potent and orally active PCSK9 inhibitor with an IC50 value of 6.4 µM. PCSK9-IN-10 enhances the expression of LDLR protein while reducing PCSK9 expression. PCSK9-IN-10 demonstrates efficacy in reducing the progression of atherosclerosis and holds promise for research on hyperlipidemia [1]. |
体内研究 | Administration of PCSK9-IN-10 at a dose of 30 mg/kg orally once a day for 8 weeks results in reductions in total cholesterol (TC) levels and atherosclerotic plaque size in ApoE knockout mice [1]. |
体外研究 | Exposure to PCSK9-IN-10 at concentrations ranging from 0 to 25 µM for 24 hours significantly decreases PCSK9 protein expression and increases LDL receptor (LDLR) expression in a dose-dependent manner [1]. |
计算器 | ||||
存储液制备 | 1mg | 5mg | 10mg | |
1 mM 5 mM 10 mM |
2.68mL 0.54mL 0.27mL |
13.39mL 2.68mL 1.34mL |
26.78mL 5.36mL 2.68mL |
CAS号 | 368434-98-4 |
分子式 | C18H23N5O4 |
分子量 | 373.406 |
别名 | |
运输 | 蓝冰 |
存储条件 |
液体 -20°C:3-6个月-80°C:12个月 粉末 Inert atmosphere,2-8°C |
溶解度 |
DMSO: 250 mg/mL(669.51 mM),配合低频超声助溶,注意:DMSO长时间开封后,会吸水并导致溶解能力下降,请避免使用长期开封的DMSO |
动物实验配方 |