1. Metabolic Enzyme/Protease
  2. ANGPTL PCSK9
  3. DC371739

DC371739 是一种有效的,具有口服活性的 PCSK9 抑制剂。DC371739 可降低 PCSK9 和 ANGPTL3 的 mRNA 表达。DC371739 可降低 PCSK9 的蛋白表达并增加 LDLR 的蛋白表达。DC371739 具有用于高脂血症研究的潜力。

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DC371739 Chemical Structure

DC371739 Chemical Structure

CAS No. : 2135765-21-6

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查看 ANGPTL 亚型特异性产品:

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  • 参考文献

生物活性

DC371739 is a potent and orally activity PCSK9 inhibitor. DC371739 decreases the mRNA expression of PCSK9 and ANGPTL3. DC371739 decreases the protein expression of PCSK9 and increases the protein expression of LDLR. DC371739 has the potential for the research of hyperlipidemia[1][2].

体外研究
(In Vitro)

DC371739 (0-10 µM, 0-24 h) 以剂量和时间依赖的方式增加 HepG2 细胞中 DiI-LDL 摄取率[2]
DC371739 (0-5 µM; 4, 24, 48 h) 降低 HepG2 细胞中 PCSK9 和 ANGPTL3 的 mRNA 表达[2]
DC371739 (0-10 µM;24 h) 降低 PCSK9 的蛋白质表达并增加 LDLR 的蛋白质表达[2]
DC371739 (5µM; 24 h) 通过靶向 HNF-1α 抑制 ANGPTL3 转录和表达[2]

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

RT-PCR[2]

Cell Line: HepG2 cells
Concentration: 0-5 µM
Incubation Time: 4, 24, 48 h
Result: Decreased the mRNA expression of PCSK9 and ANGPTL3 in a dose and time dependent manner.

Western Blot Analysis[2]

Cell Line: HepG2, LO2 cells
Concentration: 0.5, 1, 2.5, 5, 10 µM
Incubation Time: 24 h
Result: Decreased the protein expression of PCSK9 and increased the protein expression of LDLR in a dose-dependent manner.
体内研究
(In Vivo)

DC371739 (10, 30, 100 mg/kg; p.o.; daily for 21 days) 可降低仓鼠血浆中总胆固醇 (TC)、低密度脂蛋白胆固醇 (LDL-C) 和甘油三酯的水平[2]

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Six-week-old healthy male Syrian golden hamsters (HFD-fed) [2]
Dosage: 10, 30, 100 mg/kg
Administration: P.o.; daily for 21 days
Result: Decreased the serum TC levels of the hamsters treated with 10, 30, or 100 mg/kg by 29.46%, 35.65%, and 38.69%, the serum LDL-C levels were significantly lower by 23.25%, 31.04%, and 35.03%, respectively, led to significantly lower serum TG levels by 49.57%, 57.52%, and 78.16%.
分子量

470.56

Formula

C29H30N2O4

CAS 号
运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.

纯度 & 产品资料
参考文献
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  • 稀释计算器

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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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DC371739
目录号:
HY-163794
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