1. Metabolic Enzyme/Protease
  2. CETP
  3. Anacetrapib

Anacetrapib  (Synonyms: 安塞曲匹; MK-0859)

目录号: HY-12090 纯度: 98.78%
COA 产品使用指南

Anacetrapib 是一种有效的 CETP 抑制剂,作用于 rhCETP 和 C13S CETP 突变型,IC50 分别为 7.9±2.5 nM 和 11.8±1.9 nM。

MCE 的所有产品仅用作科学研究或药证申报,我们不为任何个人用途提供产品和服务

我们将采用定制合成服务的方式为您快速提供所需产品和技术服务

Anacetrapib Chemical Structure

Anacetrapib Chemical Structure

CAS No. : 875446-37-0

1.  客户无需承担相应的运输费用。

2.  同一机构(单位)同一产品试用装仅限申领一次,同一机构(单位)一年内

     可免费申领三个不同产品的试用装。

3.  试用装只面向终端客户

规格 价格 是否有货 数量
Free Sample (0.1 - 0.2 mg)   Apply now  
10 mM * 1 mL in DMSO ¥1122
In-stock
5 mg ¥800
In-stock
10 mg ¥1280
In-stock
50 mg ¥3800
In-stock
100 mg ¥5550
In-stock
200 mg   询价  
500 mg   询价  

* Please select Quantity before adding items.

Customer Review

注册 MCE会员完成审核
即刻享有 积分商城 300 专属积分

Top Publications Citing Use of Products

    Anacetrapib purchased from MCE. Usage Cited in: Diabetes. 2018 Dec;67(12):2494-2506.  [Abstract]

    Western blots for CETP and SAA1 proteins in serum. Membrane for SAA1 are stripped and re-probed with the PLTP antibody. Molecular weight positions (BioRad precision plus protein kaleidoscope standards) are shown on the right side of blots.
    • 生物活性

    • 实验参考方法

    • 纯度 & 产品资料

    • 参考文献

    生物活性

    Anacetrapib is a potent CETP inhibitor, with IC50s of 7.9±2.5 nM and 11.8±1.9 nM for rhCETP and C13S CETP mutant, respectively.

    IC50 & Target

    IC50: 7.9±2.5 nM (rhCETP), 11.8±1.9 nM (CETPC13S)[1]

    体外研究
    (In Vitro)

    Anacetrapib dose-dependently and significantly decreases the transfer of CE from HDL3 to HDL2 (P<0.001 for concentrations equal to and higher than 0.1 µM). Excess Anacetrapib (25 µM) decreases the amount of [14C]Torcetrapib (0.25 µM) binds to immobilized rhCETP by 82% and 60%, respectively. Anacetrapib decreases pre-β-HDL formation by more than 46% (P<0.001) at all concentrations tested (0.1, 1, 3, and 10 µM)[1]. A significant reduction of PCSK9 promoter activity by Anacetrapib (ANA) is detected at 3 µM concentration (−22%, p<0.01) and further lowered to 68% of control at 10 µM. Likewise, luciferase activity of B11 cells are decreased by Anacetrapib at 3 µM concentration and reached to a maximal reduction of 38% of control at 10 µM. At 10 µM concentration, Anacetrapib loweres PCSK9 mRNA level to 60% of control and LDLR mRNA level to 67% of control[2].

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

    体内研究
    (In Vivo)

    Hamsters are given Anacetrapib for 7 days before injection of [3H]cholesterol-labeled macrophages (day 0). Treatment with Anacetrapib leads to significant increases in HDL-C levels at day 0. At day 3, [3H]cholesterol radioactivity in the HDL fraction is significantly increased from control values for Anacetrapib[1]. Anacetrapib (ANA) treatment modestly elevates serum total serum cholesterol levels ~10% (p<0.05) and increases serum LDL-C by 26% (p<0.05) as compared to vehicle control[2]. After an intravenous dose of 0.5 mg/kg, the mean values for systemic plasma clearance, steady-state volume of distribution, and terminal half-life are 2.3 mL/min/kg, 1.1 L/kg, and 12 h, respectively. After oral dosing at 5 mg/kg, the bioavailability of Anacetrapib is 38%. Exposures (AUC) increases in a less than dose-proportional manner from 23 μM•h at 5 mg/kg to 362 μM•h at 500 mg/kg. In this dose range, the peak plasma level (Cmax) ranges from 5 to 26 μM and the time to reach peak plasma level (Tmax) ranged from 3 to 4.5 h[3].

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

    Clinical Trial
    分子量

    637.51

    Formula

    C30H25F10NO3

    CAS 号
    性状

    固体

    颜色

    White to off-white

    中文名称

    安塞曲匹;安塞曲比;安塞曲贝

    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 2 years
    -20°C 1 year
    溶解性数据
    In Vitro: 

    DMSO 中的溶解度 : ≥ 100 mg/mL (156.86 mM; 吸湿的 DMSO 对产品的溶解度有显著影响,请使用新开封的 DMSO)

    * "≥" means soluble, but saturation unknown.

    配制储备液
    浓度 溶剂体积 质量 1 mg 5 mg 10 mg
    1 mM 1.5686 mL 7.8430 mL 15.6860 mL
    5 mM 0.3137 mL 1.5686 mL 3.1372 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, 2 years; -20°C, 1 year。-80°C储存时,请在2年内使用, -20°C储存时,请在1年内使用。

    • 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: ≥ 2.75 mg/mL (4.31 mM); 澄清溶液

      此方案可获得 ≥ 2.75 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 27.5 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)。
    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: 98.78%

    参考文献
    Kinase Assay
    [1]

    The inhibitory potency (IC50) of Dalcetrapib, Torcetrapib, and Anacetrapib to decrease CE transfer from HDL to LDL by rhCETP and C13S CETP is measured using a scintillation proximity assay kit. Briefly, [3H]CE-labeled HDL donor particles are incubated in the presence of purified CETP proteins (final concentration 0.5 µg/mL) and biotinylated LDL acceptor particles for 3 h at 37°C. Subsequently, streptavidin-coupled polyvinyltoluene beads containing liquid scintillation cocktail binding selectively to biotinylated LDL are added, and the amount of [3H]CE molecules transferred to LDL is measured by β counting[1].

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

    Cell Assay
    [2]

    Cells are seeded in a 96 well plate overnight prior to the treatment by different concentrations of CETP inhibitors (e.g., Anacetrapib) for 24 h. Cell viability is measured using the CellTiter-Glo Luminescent Cell Viability Assay kit. Four wells are evaluated under each experimental condition[2].

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

    Animal Administration
    [2][3]

    Mice[2]
    Eight-week old male C57BL/6J mice are housed (4 animals/cage) under controlled temperature (72°F) and lighting (12 h light/dark cycle). Animals have free access to autoclaved water and food. In the first in vivo study, after an acclimatization period of 7 days, mice are fed a high-fat high-cholesterol diet (HFHC) containing 35% calories from fat and 1.25% cholesterol for two weeks. Mice are then divided into two groups (n=8 per group) and are given a daily dose of Anacetrapib at 50 mg/kg by oral gavage. The control group receive vehicle (0.5% methyl cellulose). The drug treatment lasts 7 days. In the second in vivo study, mice fed a normal chow diet are treated with Anacetrapib (50 mg/kg, n=8) or vehicle (n=8) for 10 days. Serum samples are collected after a 4 h fasting before and after the drug treatment. After the last dosing, all animals are sacrificed for collection of serum and liver tissues. Livers are immediately removed, cut into small pieces, and stored at −80°C for RNA and protein isolations and cholesterol measurement.
    Rats[3]
    Adult male Sprague-Dawley rats, weighing 280 to 330 g, are fasted overnight before the study. The animals are allowed access to food 4 h after dosing, but water is provided ad libitum. For intravenous administration, four rats received a dose of Anacetrapib (dosing volume 2.5 mL/kg) via bolus injection through a catheter previously implanted into the femoral vein, followed by a 300 μL saline flush. The intravenous dose of Anacetrapib is formulated in polyethylene glycol 300-water (7:3, v/v) at a concentration of 0.2 mg/mL. For oral administration, four rats received a dose via oral gavage (dosing volume 2 mL/kg). These oral doses of 5, 50, 100, and 500 mg/kg are formulated in Imwitor 742-Tween 80 (1:1, w/w) at concentrations of 2.5, 25, 50, and 250 mg/mL, respectively. Blood samples (0.3 mL) are collected into EDTA-containing tubes at the following time points: predose and 0.083 (intravenous only), 0.25, 0.5, 1, 2, 4, 6, 8, 24, and 48 h postdose. Blood samples are stored on ice, and plasma is prepared by centrifugation. Plasma is transferred to a 96-well plate and stored at −70°C until analysis.

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

    参考文献

    Anacetrapib 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, 2 years; -20°C, 1 year。-80°C储存时,请在2年内使用, -20°C储存时,请在1年内使用。

    可选溶剂 浓度 溶剂体积 质量 1 mg 5 mg 10 mg 25 mg
    DMSO 1 mM 1.5686 mL 7.8430 mL 15.6860 mL 39.2151 mL
    5 mM 0.3137 mL 1.5686 mL 3.1372 mL 7.8430 mL
    10 mM 0.1569 mL 0.7843 mL 1.5686 mL 3.9215 mL
    15 mM 0.1046 mL 0.5229 mL 1.0457 mL 2.6143 mL
    20 mM 0.0784 mL 0.3922 mL 0.7843 mL 1.9608 mL
    25 mM 0.0627 mL 0.3137 mL 0.6274 mL 1.5686 mL
    30 mM 0.0523 mL 0.2614 mL 0.5229 mL 1.3072 mL
    40 mM 0.0392 mL 0.1961 mL 0.3922 mL 0.9804 mL
    50 mM 0.0314 mL 0.1569 mL 0.3137 mL 0.7843 mL
    60 mM 0.0261 mL 0.1307 mL 0.2614 mL 0.6536 mL
    80 mM 0.0196 mL 0.0980 mL 0.1961 mL 0.4902 mL
    100 mM 0.0157 mL 0.0784 mL 0.1569 mL 0.3922 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.

    您最近查看的产品:

    Your information is safe with us. * Required Fields.

       产品名称:

     

    * 需求量:

    * 客户姓名:

     

    * Email:

    * 电话:

     

    * 公司或机构名称:

       留言给我们:

    Bulk Inquiry

    Inquiry Information

    产品名称:
    Anacetrapib
    目录号:
    HY-12090
    需求量: