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

Anacetrapib (Synonyms: MK-0859)

製品番号: HY-12090 純度: 98.39%
取扱説明書

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.

商品は「研究用試薬」です。人や動物の医療用・臨床診断用・食品用としては使用しないように、十分ご注意ください。

Anacetrapib 構造式

Anacetrapib 構造式

CAS 番号 : 875446-37-0

容量 価格(税別) 在庫状況 数量
無料サンプル (0.5-1 mg)   今すぐ申し込む  
10 mM * 1 mL in DMSO USD 168 在庫あり
Estimated Time of Arrival: December 31
5 mg USD 120 在庫あり
Estimated Time of Arrival: December 31
10 mg USD 200 在庫あり
Estimated Time of Arrival: December 31
50 mg USD 580 在庫あり
Estimated Time of Arrival: December 31
100 mg USD 880 在庫あり
Estimated Time of Arrival: December 31
200 mg   お問い合わせ  
500 mg   お問い合わせ  

* アイテムを追加する前、数量をご選択ください

カスタマーレビュー

Based on 3 publication(s) in Google Scholar

Top Publications Citing Use of Products

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

    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

    • プロトコル

    • 純度とドキュメンテーション

    • 参考文献

    • カスタマーレビュー

    製品説明

    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]

    体外実験

    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].

    体内実験

    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].

    臨床実験
    分子量

    637.51

    分子式

    C₃₀H₂₅F₁₀NO₃

    CAS 番号

    875446-37-0

    SMILES

    O=C1O[[email protected]@H]([[email protected]@H](N1CC2=CC(C(F)(F)F)=CC=C2C3=CC(C(C)C)=C(C=C3OC)F)C)C4=CC(C(F)(F)F)=CC(C(F)(F)F)=C4

    輸送条件

    Room temperature in continental US; may vary elsewhere.

    保管条件
    Powder -20°C 3 years
      4°C 2 years
    In solvent -80°C 6 months
      -20°C 1 month
    溶剤 & 溶解度
    体外: 

    DMSO : ≥ 100 mg/mL (156.86 mM)

    H2O : < 0.1 mg/mL (insoluble)

    *"≥" means soluble, but saturation unknown.

    Preparing
    Stock Solutions
    Concentration Solvent Mass 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
    10 mM 0.1569 mL 0.7843 mL 1.5686 mL
    *Please refer to the solubility information to select the appropriate solvent.
    体内:
    • 1.

      Add each solvent one by one:  10% DMSO    90% corn oil

      Solubility: ≥ 2.75 mg/mL (4.31 mM); Clear solution

    *All of the co-solvents are provided by MCE.
    参考文献
    キナーゼ実験
    [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 はこれらの方法の精度を確認していません。 こちらは参照専用です。

    細胞実験
    [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 はこれらの方法の精度を確認していません。 こちらは参照専用です。

    動物実験
    [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 はこれらの方法の精度を確認していません。 こちらは参照専用です。

    参考文献
    • No file chosen (Maximum size is: 1024 Kb)
    • If you have published this work, please enter the PubMed ID.
    • Your name will appear on the site.
    • モル濃度カルキュレーター

    • 希釈カルキュレーター

    The molarity calculator equation

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

    Mass   Concentration   Volume   Molecular Weight *
    = × ×

    The dilution calculator equation

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

    This equation is commonly abbreviated as: C1V1 = C2V2

    Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
    × = ×
    C1   V1   C2   V2

    Keywords:

    AnacetrapibMK-0859MK0859MK 0859CETPCholesteryl ester transfer proteinInhibitorinhibitorinhibit

    最近チェックした製品:

    オンラインお問い合わせ

    Your information is safe with us. * Required Fields.

    製品名

     

    タイトル

    お名前 *

     

    PC 用メールアドレス *

    電話番号 *

     

    勤務先/学校名 *

    国会或いは地域 *

     

    カスタマ需要量 *

    必ず会社名を記載ください。個人への返信は行いません。

    メッセージ

    バルクお問い合わせ

    Inquiry Information

    製品名:
    Anacetrapib
    製品番号:
    HY-12090
    数量:
    MCE 日本正規代理店: