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PCSK9-IN-11

CAS No. :

MCE 国际站：PCSK9-IN-11

产品活性：PCSK9-IN-11 (compound 5r) 是一种口服有效的 PCSK9 抑制剂。 PCSK9-IN-11 在 HepG2 细胞中表现出 PCSK9 转录抑制活性，IC₅₀ 为 5.7 μM。 PCSK9-IN-11 增加 LDL 受体 (LDLR) 蛋白水平。 PCSK9-IN-11 可用于动脉粥样硬化研究。

研究领域：Metabolic Enzyme/Protease

作用靶点：Ser/Thr Protease

In Vitro: PCSK9-IN-11 (compound 5r) (0-25 μM, 24 h) significantly decreases PCSK9 protein level and increases LDLR expression in a dose dependent manner.

In Vivo: PCSK9-IN-11 (compound 5r) (0-1000 mg/kg, IG, once) exhibits a good in vivo safety feature with the halflethal dose (LD₅₀) value of over 1000 mg/kg.
PCSK9-IN-11 (30 mg/kg, IG, once a day for 8 weeks) significantly suppresses hepatic PCSK9 expression and slightly reduces serum PCSK9 level.

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