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 PCSK9ANGPTL3mRNA 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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10 mg ¥2350
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25 mg ¥4690
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Customer Review

查看 ANGPTL 亚型特异性产品:

  • 生物活性

  • 纯度 & 产品资料

  • 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 PCSK9ANGPTL3mRNA 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
性状

固体

颜色

Light yellow to light brown

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
溶解性数据
细胞实验: 

DMSO 中的溶解度 : 25 mg/mL (53.13 mM; 超声助溶; 吸湿的 DMSO 对产品的溶解度有显著影响,请使用新开封的 DMSO)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 2.1251 mL 10.6256 mL 21.2513 mL
5 mM 0.4250 mL 2.1251 mL 4.2503 mL
查看完整储备液配制表

* 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效
储备液的保存方式和期限:-80°C, 6 months; -20°C, 1 month。-80°C储存时,请在6个月内使用,-20°C储存时,请在1个月内使用。

  • 摩尔计算器

  • 稀释计算器

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

质量
=
浓度
×
体积
×
分子量 *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

浓度 (start)

C1

×
体积 (start)

V1

=
浓度 (final)

C2

×
体积 (final)

V2

动物溶解方案计算器
请输入动物实验的基本信息:

给药剂量

mg/kg

动物的平均体重

g

每只动物的给药体积

μL

动物数量

由于实验过程有损耗,建议您多配一只动物的量
计算结果
工作液所需浓度 : mg/mL
纯度 & 产品资料
参考文献

完整储备液配制表

* 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效
储备液的保存方式和期限:-80°C, 6 months; -20°C, 1 month。-80°C储存时,请在6个月内使用,-20°C储存时,请在1个月内使用。

可选溶剂 浓度 溶剂体积 质量 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.1251 mL 10.6256 mL 21.2513 mL 53.1282 mL
5 mM 0.4250 mL 2.1251 mL 4.2503 mL 10.6256 mL
10 mM 0.2125 mL 1.0626 mL 2.1251 mL 5.3128 mL
15 mM 0.1417 mL 0.7084 mL 1.4168 mL 3.5419 mL
20 mM 0.1063 mL 0.5313 mL 1.0626 mL 2.6564 mL
25 mM 0.0850 mL 0.4250 mL 0.8501 mL 2.1251 mL
30 mM 0.0708 mL 0.3542 mL 0.7084 mL 1.7709 mL
40 mM 0.0531 mL 0.2656 mL 0.5313 mL 1.3282 mL
50 mM 0.0425 mL 0.2125 mL 0.4250 mL 1.0626 mL
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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产品名称:
DC371739
目录号:
HY-163794
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