2. Metabolic Enzyme/Protease
  3. CETP
  4. Evacetrapib

Evacetrapib  (Synonyms: LY2484595)

製品番号: HY-13327 純度: 99.38%
COA 取扱説明書 Technical Support

Evacetrapib is a potent and selective of CETP inhibitor, which inhibits human recombinant CETP protein (IC50 5.5 nM) and CETP activity in human plasma (IC50 36 nM) in vitro.

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CAS 番号 : 1186486-62-3

容量 価格（税別） 在庫状況 数量
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
 USD 91 在庫あり
Solution
10 mM * 1 mL in DMSO USD 91 在庫あり
Solid
5 mg $65 在庫あり
10 mg $110 在庫あり
25 mg $245 在庫あり
50 mg $420 在庫あり
100 mg $720 在庫あり
200 mg   お問い合わせ  
500 mg   お問い合わせ  

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Based on 3 publication(s) in Google Scholar

Other Forms of Evacetrapib:

Evacetrapib 関連抗体

Top Publications Citing Use of Products

    Evacetrapib purchased from MedChemExpress. Usage Cited in: Atherosclerosis. 2014 Aug;235(2):449-62.  [Abstract]

    Downregulation of SREBP2-M by EVA and TOR reduced LDLR and PCSK9 expression. HepG2 cells are treated with EVA at indicated concentrations for 24 h. Total cell lysates (30 µg) are analyzed for the protein abundance of LDLR and β-actin. Nuclear and cytoplasmic extracts are isolated from each sample. Nuclear extracts of 30 µg protein per sample are used to detect SREBP2-M. The membrane is reprobed with anti-HDAC1. Cytoplasmic extracts of 30 µg protein per sample are used to detect SREBP2-P. The mem

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    製品説明

    Evacetrapib is a potent and selective of CETP inhibitor, which inhibits human recombinant CETP protein (IC50 5.5 nM) and CETP activity in human plasma (IC50 36 nM) in vitro.

    IC50 & Target

    IC50: 5.5 nM (CETP)[1]
    体外実験

    Evacetrapib is a novel benzazepine-based CETP inhibitor. In the buffer CETP assay, the absolute potency of the compound is 5.5 nM. In the human plasma CETP assay, the CETP concentration is about 2 μg/mL (25 nM) and the 36 nM IC50 value again indicates that Evacetrapib is a potent CETP inhibitor against either the recombinant protein or CETP from human plasma. Evacetrapib is apparently much more potent than Dalcetrapib[1].

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

    Evacetrapib 関連抗体
    体内実験

    In double transgenic mice expressing human CETP and apoAI, Evacetrapib exhibits an ex vivo CETP inhibition ED50 of less than 5 mg/kg at 8 h post oral dose and significantly elevated HDL cholesterol. Importantly, no blood pressure elevation is observed in rats dosed with Evacetrapib at high exposure multiples compared with the positive control, torcetrapib. Evacetrapib administered orally at 30 mg/kg results in 98.4%, 98.6%, and 18.4% inhibition of CETP activity at 4, 8 and 24 h post dose respectively. Evacetrapib dosed orally at 30 mg/kg resulted in 129.7% increase in HDL-C 8 h after oral administration[1].

    MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
    臨床実験
    分子量

    638.65

    分子式

    C31H36F6N6O2
    CAS 番号
    Appearance

    Solid

    Color

    White to light yellow

    SMILES

    O=C([C@H]1CC[C@H](CN2CCC[C@H](N(CC3=CC(C(F)(F)F)=CC(C(F)(F)F)=C3)C4=NN(C)N=N4)C5=CC(C)=CC(C)=C52)CC1)O
    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 (156.58 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

    *"≥" means soluble, but saturation unknown.

    Preparing
    Stock Solutions
    Concentration Solvent Mass 1 mg 5 mg 10 mg
    1 mM 1.5658 mL 7.8290 mL 15.6580 mL
    5 mM 0.3132 mL 1.5658 mL 3.1316 mL
    10 mM 0.1566 mL 0.7829 mL 1.5658 mL
    View the Complete Stock Solution Preparation Table

    * Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
    Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

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

    一般には略語で表示されます：C1V1 = C2V2

    濃度 （開始）

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    体内:

    Select the appropriate dissolution method based on your experimental animal and administration route.

    For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
    To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
    The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

    • Protocol 1

      Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% Saline

      Solubility: ≥ 2.5 mg/mL (3.91 mM); Clear solution

      This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

      Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
    • Protocol 2

      Add each solvent one by one:  10% DMSO    90% Corn Oil

      Solubility: ≥ 2.5 mg/mL (3.91 mM); Clear solution

      This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

    In Vivo Dissolution Calculator
    Please enter the basic information of animal experiments:

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    Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
    Please enter your animal formula composition:
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    Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
    The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
    Calculation results:
    Working solution concentration: mg/mL
    Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
    The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
    Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
     If the continuous dosing period exceeds half a month, please choose this protocol carefully.
    Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
    純度とドキュメンテーション
    参考文献
    キナーゼ実験
    [1]

    Human CETP cDNA is amplified from a human liver cDNA library and the sequence is confirmed to be identical to the published sequence. The cDNA is subcloned into a pcDNA3.1 vector, under the control of CMV promoter. A stable line is established in CV1 cells in which the above-mentioned construct is used to express the recombinant human CETP. The medium contained the secreted recombinant CETP protein and the amount (19 ng/μL) is quantified by an ELISA kit. The medium is then aliquoted in 0.2% BSA and stored at -80°C. The stock CETP protein is diluted 150-fold in CETP buffer (10 mM Tris, 150 mM NaCl, and 2 mM EDTA) before use. The assay is set up in a 96-well plate. Each well received 97.5 μL diluted CETP protein (final concentration 7 nM) and 2.5 μL of compound stock. After a 30 min incubation at 37°C, 5 μL of substrate stock (the same stock used in the human plasma CETP assay), 0.16 μL of VLDL stock (2.5 mg/mL, Intracel) and 145 μL of CETP buffer are added, and the incubation is continued for another 4 h. Signal is read for the human plasma CETP assay[1].

    MedChemExpress (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
    [1]

    Rats[1]
    The blood pressure study is carried out using telemetered, male, obese Zucker Diabetic rats (ZDF fa/fa rats, 8 weeks of age on arrival; n=4). All rats underwent surgical implantation of a telemetry transmitter for continuous monitoring of hemodynamic parameters throughout the study. The rats are acclimated on Purina 5008 chow and house water ad libitum until 11 weeks of age. Mean daily blood pressure for the 24-h period immediately prior to administration of compound is taken as the baseline blood pressure. On the day of an experiment, a single 160 mg/kg dose (in 10% acacia) of Evacetrapib as the lysine salt is administered by oral gavage, and the drug effect is taken as the average daily mean arterial pressure (MAP) during the 24 h period following the dose. Data are expressed as the change in MAP from baseline. Following the last day of blood pressure monitoring, samples are collected from the orbital sinus at 1, 2, 4, 8, and 24 h post dose into tubes containing EDTA and processed into plasma. Plasma concentrations of Evacetrapib are measured using liquid chromatography tandem mass spectrometry.

    MedChemExpress (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

    Complete Stock Solution Preparation Table

    * Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
    Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

    Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
    DMSO 1 mM 1.5658 mL 7.8290 mL 15.6580 mL 39.1451 mL
    5 mM 0.3132 mL 1.5658 mL 3.1316 mL 7.8290 mL
    10 mM 0.1566 mL 0.7829 mL 1.5658 mL 3.9145 mL
    15 mM 0.1044 mL 0.5219 mL 1.0439 mL 2.6097 mL
    20 mM 0.0783 mL 0.3915 mL 0.7829 mL 1.9573 mL
    25 mM 0.0626 mL 0.3132 mL 0.6263 mL 1.5658 mL
    30 mM 0.0522 mL 0.2610 mL 0.5219 mL 1.3048 mL
    40 mM 0.0391 mL 0.1957 mL 0.3915 mL 0.9786 mL
    50 mM 0.0313 mL 0.1566 mL 0.3132 mL 0.7829 mL
    60 mM 0.0261 mL 0.1305 mL 0.2610 mL 0.6524 mL
    80 mM 0.0196 mL 0.0979 mL 0.1957 mL 0.4893 mL
    100 mM 0.0157 mL 0.0783 mL 0.1566 mL 0.3915 mL
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    Evacetrapib Related Classifications

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    The dilution calculator equation

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

    一般には略語で表示されます：C1V1 = C2V2

    濃度 （開始） × 体積 （開始） = 濃度 （終了） × 体積 （終了）
    × = ×
    C1   V1   C2   V2
    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:

    Evacetrapib1186486-62-3LY2484595LY 2484595LY-2484595CETPCholesteryl ester transfer proteinInhibitorinhibitorinhibit

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