2. Metabolic Enzyme/Protease
  3. ATGL
  4. Atglistatin

Atglistatin is a selective adipose triglyceride lipase (ATGL) inhibitor which inhibits lipolysis with an IC50 of 0.7 μM in vitro.

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

Atglistatin Chemical Structure

Atglistatin Chemical Structure

CAS No. : 1469924-27-3

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10 mM * 1 mL in DMSO
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Customer Review

Based on 11 publication(s) in Google Scholar

Atglistatin Related Antibodies

Top Publications Citing Use of Products

    Atglistatin purchased from MedChemExpress. Usage Cited in: Fish Physiol Biochem. 2017 Jun;43(3):813-822.  [Abstract]

    Atglistatin (HY-15859) attenuates the increase in GyK induced by EPA at 12 h. GyK gene expression and enzyme activity after hypertrophic model cells treated with 50 μM HY-15859, 100 μM EPA alone, or both for 12 h.HY-15859 is added 2 h in advance.

    • Biological Activity

    • Protocol

    • Purity & Documentation

    • References

    • Customer Review

    Description

    Atglistatin is a selective adipose triglyceride lipase (ATGL) inhibitor which inhibits lipolysis with an IC50 of 0.7 μM in vitro.

    IC50 & Target

    IC50: 0.7 μM (ATGL)[1]
    In Vitro

    Atglistatin inhibits Triacylglycerol (TG) hydrolase activity of wild-type white adipose tissue (WAT) in a dose-dependent manner up to 78% at the highest concentration. In comparison to wild-type preparations, TG hydrolase activity in WAT lysates from ATGL-ko animals is reduced by approximately 70% and Atglistatin had only a moderate effect on the residual activity. The combined use of Atglistatin and the hormone-sensitive lipase (HSL) inhibitor Hi 76-0079 leads to an almost complete inhibition (-95%) of TG hydrolase activity of WAT which implicates that most of the non-ATGL activity can be ascribed to HSL[1].

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

    Atglistatin Related Antibodies
    In Vivo

    Animals receive Atglistatin dissolved in olive oil by oral gavage. After application, blood and tissues are collected for determination of plasma parameters, tissue Triacylglycerol (TG) levels, and inhibitor concentrations. Time-course experiments revealed that the lipolytic parameters fatty acids (FA) and glycerol are reduced 4 and 8 hours after application and returned to normal after 12 hours. Eight hours after treatment, a dose-dependent decrease is observed in FA and glycerol levels up to 50% and 62%, respectively. Atglistatin also caused a strong reduction in plasma TG levels (-43%) while blood glucose, total cholesterol, ketone bodies, and insulin levels do not significantly change. Dose and time-dependent inhibition of lipolysis is also observed in response to intraperitoneal injection of Atglistatin[1].

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

    283.37

    Formula

    C17H21N3O
    CAS No.
    Appearance

    Solid

    Color

    White to yellow

    SMILES

    O=C(NC1=CC(C2=CC=C(N(C)C)C=C2)=CC=C1)N(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 2 years
    -20°C 1 year
    Solvent & Solubility
    In Vitro: 

    DMSO : ≥ 100 mg/mL (352.90 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 3.5290 mL 17.6448 mL 35.2896 mL
    5 mM 0.7058 mL 3.5290 mL 7.0579 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.

    • Molarity Calculator

    • Dilution Calculator

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

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

    This equation is commonly abbreviated as: C1V1 = C2V2

    Concentration (start)

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    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: ≥ 2.5 mg/mL (8.82 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 (8.82 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.

    For the following dissolution methods, please prepare the working solution directly. It is recommended to prepare fresh solutions and use them promptly within a short period of time.
    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:  Corn Oil

      Solubility: 6.25 mg/mL (22.06 mM); Suspended solution; Need ultrasonic

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

    Dosage

    mg/kg

    Animal weight
    (per animal)

    g

    Dosing volume
    (per animal)

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    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: 98.86%

    COA (245 KB) HNMR (407 KB) LCMS (109 KB)

    Handling Instructions (2659 KB)
    References
    Cell Assay
    [1]

    For MTT-based in vitro viability assays, cells are seeded at an initial density of 1×104 cells per well in 96-well plates and cultured under standard conditions for 24 hours. The next day, cells are pretreated with different concentrations of Atglistatin dissolved in DMSO or Cisplatin dissolved in dimethylformamide (DMF) as positive control for two hours. Medium is replaced by an identical fresh medium and incubated again for the indicated time-points. Thereafter cells are incubated for 3 hours with 100 μL Thiazolyl Blue Tetrazolium Bromide (MTT). The resulting violet formazan crystals are dissolved by adding 100 μL of MTT solubilization solution (0.1% NP-40, 4 mM HCl and anhydrous isopropanol). After complete dissolution of the formazan product, absorbance is measured at 595 nm using 690 nm as reference wavelength[1].

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.
    Animal Administration
    [1]

    Mice[1]
    Mice (C57Bl/6J) are used. Atglistatin is administrated orally by gavage in olive oil (200 μL) or by IP injection. For IP administration, we generated Atglistatin hydrochloride by the addition of 25 % HCl resulting in a water soluble compound. For intraperitoneal injection the inhibitor is dried, excess HCl is buffered with Tris base, and Atglistatin is dissolved in PBS containing 0.25 % Cremophor EL (pH 7.1). Atglistatin is administered orally by gavage in olive oil (1.4 mg/mouse). After 8 h tissues are collected and extracted twice using Folch procedure. Combined organic phases are concentrated, reconstituted in 500 μL chloroform and ssubjected to solid phase extraction (SPE). For SPE samples are loaded onto silica columns washed twice with 2 mL of chloroform and Atglistatin is eluted using 3 mL chloroform/methanol (99/1, v/v). Eluted samples are concentrated, dissolved in n-propanol/chloroform/methanol (8/1.3/0.6, v/v/v) and analyzed by UPLC/MS (m/z 284, MH+; SYNAPT G1 qTOF HD mass spectrometer, Waters).

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.
    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, 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 3.5290 mL 17.6448 mL 35.2896 mL 88.2239 mL
    5 mM 0.7058 mL 3.5290 mL 7.0579 mL 17.6448 mL
    10 mM 0.3529 mL 1.7645 mL 3.5290 mL 8.8224 mL
    15 mM 0.2353 mL 1.1763 mL 2.3526 mL 5.8816 mL
    20 mM 0.1764 mL 0.8822 mL 1.7645 mL 4.4112 mL
    25 mM 0.1412 mL 0.7058 mL 1.4116 mL 3.5290 mL
    30 mM 0.1176 mL 0.5882 mL 1.1763 mL 2.9408 mL
    40 mM 0.0882 mL 0.4411 mL 0.8822 mL 2.2056 mL
    50 mM 0.0706 mL 0.3529 mL 0.7058 mL 1.7645 mL
    60 mM 0.0588 mL 0.2941 mL 0.5882 mL 1.4704 mL
    80 mM 0.0441 mL 0.2206 mL 0.4411 mL 1.1028 mL
    100 mM 0.0353 mL 0.1764 mL 0.3529 mL 0.8822 mL
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    Atglistatin Related Classifications

    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:

    Atglistatin1469924-27-3ATGLAdipose triglyceride lipaseInhibitorinhibitorinhibit

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