PCSK9-IN-10

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

PCSK9-IN-10 是一种有效的，具有口服活性的 PCSK9 抑制剂，IC50 值为 6.4 μM。PCSK9-IN-10 增加 LDLR 蛋白的表达并降低 PCSK9 的表达。PCSK9-IN-10 可减缓动脉粥样硬化进展。PCSK9-IN-10 具有研究高脂血症的潜力。

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.

Cell Cytotoxicity Assay Cell Line:HepG2 cells Concentration:0-1000 μM Incubation Time:24 h Result:Showed low cytotoxicity to HepG2 cells.Western Blot Analysis Cell Line:HepG2 cells Concentration:0, 2.5, 5, 12.5, 25 μM Incubation Time:24 h Result:Significantly decreased PCSK9 protein level in a dose dependent manner.

Animal Model:Eight weeks old male ApoE KO miceDosage: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.

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Apoptosis

Serine/threonin kinase

Serine/threonin kinase

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368434-98-4

373.41

C18H23N5O4

>98% (HPLC)

In Vitro:?DMSO 中的溶解度 : 250 mg/mL (669.51 mM; 超声助溶 )

COCCNc1nc2n(C)c(=O)n(C)c(=O)c2n1Cc1cccc(OC)c1

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(-20℃)

With Ice Pack

≥ 2 years