2. Metabolic Enzyme/Protease
  3. PCSK9
  4. PCSK9-IN-11

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。

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PCSK9-IN-11 Chemical Structure

PCSK9-IN-11 Chemical Structure

CAS No. : 2882035-56-3

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25 mg ￥2000
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50 mg ￥3200
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100 mg ￥5000
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Customer Review

PCSK9-IN-11 相关抗体

Top Publications Citing Use of Products

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

PCSK9-IN-11 (compound 5r) is a potent and orally active PCSK9 inhibitor. PCSK9-IN-11 exhibits PCSK9 transcriptional inhibitory activity in HepG2 cells, with an IC50 of 5.7 μM. PCSK9-IN-11 increases LDL receptor (LDLR) protein level. PCSK9-IN-11 can be used for atherosclerosis research[1].

IC50 & Target

IC50: 5.7 μM (PCSK9)[1]
体外研究
(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[1].

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

PCSK9-IN-11 相关抗体:

Western Blot Analysis[1]

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. Markedly increased LDLR expression in a dose dependent manner. Significantly and dose-dependently increased DiI-LDL uptake by around 1.7 folds.
体内研究
(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[1].
PCSK9-IN-11 (30 mg/kg, IG, once a day for 8 weeks) significantly suppresses hepatic PCSK9 expression and slightly reduces serum PCSK9 level[1].

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

Animal Model: C57BL/6J mice[1]
Dosage: 0, 250, 500 or 1000 mg/kg
Administration: Intragastrically administrated, single dose
Result: Exhibited a good in vivo safety feature with the halflethal dose (LD50) value of over 1000 mg/kg. Did not affected the body weight, behavioral and survival characteristics of mice.
Animal Model: ApoE KO mice (under high-fat diet (HFD))[1]
Dosage: 30 mg/kg
Administration: Intragastric administration, once a day for 8 weeks
Result: Significantly suppressed hepatic PCSK9 expression and slightly reduced serum PCSK9 level.
分子量

381.79

Formula

C16H17ClFN5O3
CAS 号
性状

固体

颜色

White to off-white

运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

4°C, protect from light

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

溶解性数据
细胞实验： 

DMSO 中的溶解度 : 125 mg/mL (327.41 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 2.6192 mL 13.0962 mL 26.1924 mL
5 mM 0.5238 mL 2.6192 mL 5.2385 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 (protect from light)。-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

只
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

PCSK9-IN-11 相关分类

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 (protect from light)。-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 2.6192 mL 13.0962 mL 26.1924 mL 65.4810 mL
5 mM 0.5238 mL 2.6192 mL 5.2385 mL 13.0962 mL
10 mM 0.2619 mL 1.3096 mL 2.6192 mL 6.5481 mL
15 mM 0.1746 mL 0.8731 mL 1.7462 mL 4.3654 mL
20 mM 0.1310 mL 0.6548 mL 1.3096 mL 3.2741 mL
25 mM 0.1048 mL 0.5238 mL 1.0477 mL 2.6192 mL
30 mM 0.0873 mL 0.4365 mL 0.8731 mL 2.1827 mL
40 mM 0.0655 mL 0.3274 mL 0.6548 mL 1.6370 mL
50 mM 0.0524 mL 0.2619 mL 0.5238 mL 1.3096 mL
60 mM 0.0437 mL 0.2183 mL 0.4365 mL 1.0914 mL
80 mM 0.0327 mL 0.1637 mL 0.3274 mL 0.8185 mL
100 mM 0.0262 mL 0.1310 mL 0.2619 mL 0.6548 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.

Keywords:

PCSK9-IN-112882035-56-3PCSK9Proprotein convertase subtilisin/kexin type 9CSK9Transcriptional inhibitionCholesterolAtherosclerosisHepG2 cellsInhibitorinhibitorinhibit

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