1. Metabolic Enzyme/Protease
  2. Acyltransferase
  3. Avasimibe

Avasimibe  (Synonyms: CI-1011; PD-148515)

Cat. No.: HY-13215 Purity: 99.50%
COA Handling Instructions

Avasimibe (CI-1011; PD-148515) is an orally active acyl coenzyme A-cholesterol acyltransferase (ACAT; also called SOAT)) inhibitor with IC50s of 24 and 9.2 µM for ACAT1 and ACAT2, respectively. Avasimibe can be used for the research of prostate cancer.

For research use only. We do not sell to patients.

Avasimibe Chemical Structure

Avasimibe Chemical Structure

CAS No. : 166518-60-1

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Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
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Customer Review

Based on 11 publication(s) in Google Scholar

Top Publications Citing Use of Products

    Avasimibe purchased from MedChemExpress. Usage Cited in: Biomed Pharmacother. 2020 Oct;130:110508.  [Abstract]

    qRT-PCR data showing the expression of linc00339 in T98 G or LN229 cells treated with linc00339 plasmid, Avasimibe (7.5 μM for 48 h) alone or in combination with linc00339 plasmids.

    Avasimibe purchased from MedChemExpress. Usage Cited in: Biomed Pharmacother. 2020 Oct;130:110508.  [Abstract]

    The effect of Avasimibe on the viability of T98 G is dose-dependent and time-dependent. Similar results are found in LN229 as well. Avasimibe has an anti-tumour effect on glioma.

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    • Purity & Documentation

    • References

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    Description

    Avasimibe (CI-1011; PD-148515) is an orally active acyl coenzyme A-cholesterol acyltransferase (ACAT; also called SOAT)) inhibitor with IC50s of 24 and 9.2 µM for ACAT1 and ACAT2, respectively[1]. Avasimibe can be used for the research of prostate cancer[2].

    IC50 & Target[1]

    ACAT1

    24 μM (IC50)

    ACAT2

    9.2 μM (IC50)

    In Vitro

    Avasimibe (0, 0.25, 5, 10, 20, 40 and 80 μM; for 1, 2, and 3 days) reduces proliferation in the prostate cancer (PCa) cells[2].
    Avasimibe (10 and 20 μM; 48 h) reduces the expression of β-catenin, Vimentin, N-cadherin, Snail and MMP9, which are tightly associated with epithelial-mesenchymal transition (EMT)[2].
    Avasimibe (10 and 20 μM) trigger cell cycle arrest via the E2F-1 signalling pathway in prostate cancer. Avasimibe induces G1 phase cell cycle arrest of PCa cells[2].
    Avasimibe (10 and 20 μM) inhibits the metastasis of PCa cells[2].

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

    Cell Viability Assay[2]

    Cell Line: PCa cells (PC-3 and DU 145)
    Concentration: 0, 0.25, 5, 10, 20, 40 and 80 µM
    Incubation Time: 1, 2, and 3 days
    Result: Dose dependently inhibited PC-3 and DU 145 cell viability.

    Western Blot Analysis[2]

    Cell Line: PCa cells (PC-3 and DU 145)
    Concentration: 10 and 20 µM
    Incubation Time: 48 hours
    Result: Reduced protein levels of EMT-related proteins (β-catenin, Vimentin, N-cadherin, Snail, MMP9 and E-cadherin).

    Cell Cycle Analysis[2]

    Cell Line: PCa cells (PC-3 and DU 145)
    Concentration: 10 and 20 µM
    Incubation Time: 48 hours
    Result: Induced G1 phase cycle arrest and altered the G1 phase-related protein levels in PCa cells.
    In Vivo

    Avasimibe (30 mg/kg, intraperitoneally injected on alternate days for 7 weeks) suppresses PCa cell growth and metastasis in vivo. Avasimibe has good biocompatibility and low toxicity[2].

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

    Animal Model: SPF male mice (BALB/c-nude, 4 weeks old) bearing PCa cells[2]
    Dosage: 30 mg/kg
    Administration: Intraperitoneally injected for 7 weeks
    Result: Reduced tumour volume compared with that of the control group. Inhibited PCa growth and migration in vivo.
    Molecular Weight

    501.72

    Formula

    C29H43NO4S

    CAS No.
    Appearance

    Solid

    Color

    White to off-white

    SMILES

    O=C(NS(=O)(OC1=C(C(C)C)C=CC=C1C(C)C)=O)CC2=C(C(C)C)C=C(C(C)C)C=C2C(C)C

    Shipping

    Room temperature in continental US; may vary elsewhere.

    Storage
    Powder -20°C 3 years
    4°C 2 years
    In solvent -80°C 1 year
    -20°C 6 months
    Solvent & Solubility
    In Vitro: 

    DMSO : 100 mg/mL (199.31 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

    Preparing
    Stock Solutions
    Concentration Solvent Mass 1 mg 5 mg 10 mg
    1 mM 1.9931 mL 9.9657 mL 19.9314 mL
    5 mM 0.3986 mL 1.9931 mL 3.9863 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, 1 year; -20°C, 6 months. When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.

    • Molarity Calculator

    • Dilution Calculator

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

    Mass
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    Volume
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    Molecular Weight *

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

    This equation is commonly abbreviated as: C1V1 = C2V2

    Concentration (start)

    C1

    ×
    Volume (start)

    V1

    =
    Concentration (final)

    C2

    ×
    Volume (final)

    V2

    In Vivo:

    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: 7.5 mg/mL (14.95 mM); Suspended solution; Need ultrasonic

      This protocol yields a suspended solution of 7.5 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (75.0 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% (20% SBE-β-CD in Saline)

      Solubility: 7.5 mg/mL (14.95 mM); Suspended solution; Need ultrasonic

      This protocol yields a suspended solution of 7.5 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (75.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

      Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
    In Vivo Dissolution Calculator
    Please enter the basic information of animal experiments:

    Dosage

    mg/kg

    Animal weight
    (per animal)

    g

    Dosing volume
    (per animal)

    μL

    Number of animals

    Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
    Please enter your animal formula composition:
    %
    DMSO +
    +
    %
    Tween-80 +
    %
    Saline
    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.
    Purity & Documentation

    Purity: 99.50%

    References

    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, 1 year; -20°C, 6 months. When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.

    Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
    DMSO 1 mM 1.9931 mL 9.9657 mL 19.9314 mL 49.8286 mL
    5 mM 0.3986 mL 1.9931 mL 3.9863 mL 9.9657 mL
    10 mM 0.1993 mL 0.9966 mL 1.9931 mL 4.9829 mL
    15 mM 0.1329 mL 0.6644 mL 1.3288 mL 3.3219 mL
    20 mM 0.0997 mL 0.4983 mL 0.9966 mL 2.4914 mL
    25 mM 0.0797 mL 0.3986 mL 0.7973 mL 1.9931 mL
    30 mM 0.0664 mL 0.3322 mL 0.6644 mL 1.6610 mL
    40 mM 0.0498 mL 0.2491 mL 0.4983 mL 1.2457 mL
    50 mM 0.0399 mL 0.1993 mL 0.3986 mL 0.9966 mL
    60 mM 0.0332 mL 0.1661 mL 0.3322 mL 0.8305 mL
    80 mM 0.0249 mL 0.1246 mL 0.2491 mL 0.6229 mL
    100 mM 0.0199 mL 0.0997 mL 0.1993 mL 0.4983 mL
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    • 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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