1. Metabolic Enzyme/Protease
  2. Microsomal Triglyceride Transfer Protein (MTP)
  3. Implitapide

Implitapide  (Synonyms: 英普他派; AEGR 427)

目录号: HY-106130 纯度: 99.87%
COA 产品使用指南

Implitapide (AEGR 427) 是一种微粒体甘油三酯转移蛋白 (MTP) 抑制剂。

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Implitapide Chemical Structure

Implitapide Chemical Structure

CAS No. : 177469-96-4

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1 mg ¥3104
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5 mg ¥7760
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50 mg   询价  

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Other Forms of Implitapide:

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Top Publications Citing Use of Products
  • 生物活性

  • 实验参考方法

  • 纯度 & 产品资料

  • 参考文献

生物活性

Implitapide (AEGR 427) is a microsomal triglyceride transfer protein (MTP) inhibitor.

IC50 & Target

MTP[1]

体外研究
(In Vitro)

Implitapide suppresses MTP activity using a recombinant human form complexed with protein disulphide isomerase (IC50=10 nM) and inhibit secretion of apoB-containing very low-density lipoprotein (VLDL)-like lipoproteins from a human hepatoma cell (HepG2) with an IC50 value of 1.1 nM[1].

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

体内研究
(In Vivo)

Implitapide (3.2 mg/kg/d) significantly reduces the plasma lipid levels to nearly or below the chow diet (CD) level at 4 and 8 weeks of treatment (p<0.01). Implitapide (3.2 mg/kg/d) markedly suppresses lipid-stained lesions in the mice fed the western-type diet (WD). Implitapide (3.2 mg/kg/d) significantly decreases lesion area by 83% compared with that of the WD group (p<0.01). ApoE KO mice fed a WD containing Implitapide (1, 5, and 15 mg/kg/d) for 14 weeks have been shown to reduce significantly both plaque area (by 66, 78, and 93%, respectively) and lipid moieties within plaque (4.3, 2.6, and 0%, respectively, versus 9.5% in controls). Implitapide at a dosage of approximately 3.2 mg/kg/d significantly reduces the lipid-stained aortic lesions by 83% in apoE KO mice[1].

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

Clinical Trial
分子量

531.69

Formula

C35H37N3O2

CAS 号
性状

固体

颜色

White to off-white

中文名称

英普他派

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

-20°C, stored under nitrogen

*In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen)

溶解性数据
In Vitro: 

DMSO 中的溶解度 : 100 mg/mL (188.08 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 1.8808 mL 9.4040 mL 18.8080 mL
5 mM 0.3762 mL 1.8808 mL 3.7616 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 (stored under nitrogen)。-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

In Vivo:

请根据您的 实验动物和给药方式 选择适当的溶解方案。

以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液,再依次添加助溶剂:
——为保证实验结果的可靠性,澄清的储备液可以根据储存条件,适当保存;体内实验的工作液,建议您现用现配,当天使用
以下溶剂前显示的百分比是指该溶剂在您配制终溶液中的体积占比;如在配制过程中出现沉淀、析出现象,可以通过加热和/或超声的方式助溶

  • 方案 一

    请依序添加每种溶剂: 10% DMSO    90% Corn Oil

    Solubility: ≥ 2.5 mg/mL (4.70 mM); 澄清溶液

    此方案可获得 ≥ 2.5 mg/mL(饱和度未知)的澄清溶液,此方案实验周期在半个月以上的动物实验酌情使用。

    1 mL 工作液为例,取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中,混合均匀。

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
请输入您的动物体内配方组成:
%
DMSO +
+
%
Tween-80 +
%
Saline
如果您的动物是免疫缺陷鼠或者体弱鼠,建议 DMSO 中的在最后工作液体系中的占比尽量不超过 2%。
方案所需 助溶剂 包括:DMSO ,均可在 MCE 网站选购。 Tween 80,均可在 MCE 网站选购。
计算结果
工作液所需浓度 : mg/mL
储备液配制方法 : mg 药物溶于 μL  DMSO(母液浓度为 mg/mL)。

*In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen)

您所需的储备液浓度超过该产品的实测溶解度,以下方案仅供参考,如有需要,请与 MCE 中国技术支持联系。
动物实验体内工作液的配制方法 : 取 μL DMSO 储备液,加入 μL  μL ,混合均匀至澄清,再加 μL Tween 80,混合均匀至澄清,再加 μL 生理盐水
连续给药周期超过半月以上,请谨慎选择该方案。
请确保第一步储备液溶解至澄清状态,从左到右依次添加助溶剂。您可采用超声加热 (超声清洗仪,建议频次 20-40 kHz),涡旋吹打等方式辅助溶解。
纯度 & 产品资料

纯度: 99.87%

参考文献
Animal Administration
[1]

Mice[1]
Male apoE KO mice aged 6 weeks are fed either the CD or the WD. At age 7 weeks, apoE KO mice fed the WD are divided into two groups with similar mean body weight: apoE KO mice fed the WD and apoE KO mice fed the WD containing Implitapide (WI). Age-matched C57BL/6J mice fed the CD are used as a naive control (C57BL). Implitapide concentrations (14-22 ppm) in the diet are adjusted once a week to ensure dosage consumption of approximately 3.2 mg/kg/d. Body weight and average food consumption for 3 d are monitored weekly. Before and at 4 and 8 weeks of treatment, blood is collected for measurements of plasma lipid levels. At the 4th week, an oral fat-loading test is performed. At the 5th week of treatment, feces are collected for determination of fecal fat. At the end of 8 weeks of treatment, mice are euthanized for analysis of atherosclerotic lesions[1].

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

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 (stored under nitrogen)。-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 1.8808 mL 9.4040 mL 18.8080 mL 47.0199 mL
5 mM 0.3762 mL 1.8808 mL 3.7616 mL 9.4040 mL
10 mM 0.1881 mL 0.9404 mL 1.8808 mL 4.7020 mL
15 mM 0.1254 mL 0.6269 mL 1.2539 mL 3.1347 mL
20 mM 0.0940 mL 0.4702 mL 0.9404 mL 2.3510 mL
25 mM 0.0752 mL 0.3762 mL 0.7523 mL 1.8808 mL
30 mM 0.0627 mL 0.3135 mL 0.6269 mL 1.5673 mL
40 mM 0.0470 mL 0.2351 mL 0.4702 mL 1.1755 mL
50 mM 0.0376 mL 0.1881 mL 0.3762 mL 0.9404 mL
60 mM 0.0313 mL 0.1567 mL 0.3135 mL 0.7837 mL
80 mM 0.0235 mL 0.1175 mL 0.2351 mL 0.5877 mL
100 mM 0.0188 mL 0.0940 mL 0.1881 mL 0.4702 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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目录号:
HY-106130
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