PCSK9-IN-11|西域试剂

PCSK9-IN-11,99.66%

产品编号：Bellancom-152223| 分子式：C₁₆H₁₇ClFN₅O₃| 分子量：381.79

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货号	价格	库存与货期
Bellancom-152223	￥600.00	杭州北京（现货）
Bellancom-152223	￥1000.00	杭州北京（现货）
Bellancom-152223	￥2000.00	杭州北京（现货）
Bellancom-152223	￥3200.00	杭州北京（现货）
Bellancom-152223	￥5000.00	杭州北京（现货）

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PCSK9-IN-11

产品介绍

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。

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.

体外研究

PCSK9-IN-11 (compound 5r) (0-25 μM, 24 h) 以剂量依赖性方式显着降低 PCSK9 蛋白水平并增加 LDLR 表达。

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

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. 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，灌胃，once) 具有更好的体内安全特性，半致死剂量 (LD₅₀) 值超过 1000 mg/kg 。
PCSK9-IN-11 (30 mg/kg，灌胃，每天一次，持续 8 周) 显著抑制肝脏 PCSK9 表达并略微降低血清 PCSK9 水平。

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

Animal Model:	C57BL/6J mice
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))
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.

体内研究

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

Animal Model:	C57BL/6J mice
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))
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.

体内研究

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

Animal Model:	C57BL/6J mice
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))
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.

性状

Solid

溶解性数据

In Vitro:

DMSO : 125 mg/mL (327.41 mM; Need ultrasonic)

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
10 mM	0.2619 mL	1.3096 mL	2.6192 mL

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。

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)

参考文献