产品
编 号:F740883
分子式:C18H23N5O4
分子量:373.41
产品类型
结构图
CAS No: 368434-98-4
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产品详情
生物活性:
PCSK9-IN-10 is a potent and orally active PCSK9 inhibitor with an IC50 value of 6.4 μM. PCSK9-IN-10 increases the expression of LDLR protein and decreases the expression of PCSK9. PCSK9-IN-10 reduces atherosclerosis progression. PCSK9-IN-10 has the potential for the research of hyperlipidemia.
体内研究:
PCSK9-IN-10 (30 mg/kg;口服;每天一次,持续 8 周) 降低 ApoE KO 小鼠的总胆固醇 (TC) 和动脉粥样硬化斑块大小。Animal Model:Eight weeks old male ApoE KO mice
Dosage:30 mg/kg
Administration:P.o.; once a day for 8 weeks
Result:Inhibited both hepatic and serum PCSK9 content obviously and reduced reduced atherosclerotic plaque size.
体外研究:
PCSK9-IN-10 (compound 3s) (0, 2.5, 5, 12.5, 25 μM; 24 h) 以剂量依赖性方式显著降低 PCSK9 蛋白表达并增加 LDL 受体 (LDLR) 的表达。