1. Immunology/Inflammation NF-κB Metabolic Enzyme/Protease Membrane Transporter/Ion Channel
  2. Toll-like Receptor (TLR) MyD88 NF-κB Mitochondrial Metabolism Interleukin Related Aquaporin
  3. Atractyloside A

Atractyloside A is an orally active inhibitor of the TLR4/MyD88/NF-κB signaling pathway and also an opener of the mitochondrial permeability transition pore (MPTP). Atractyloside A interferes with the activation of the TLR4/MyD88/NF-κB pathway, thereby inhibiting intestinal inflammatory responses. Atractyloside A reverses mucin synthesis impairment, improves intestinal barrier integrity, and restores homeostasis by altering the composition of the gut microbiota. Atractyloside A can be used in studies related to spleen deficiency diarrhea and myocardial injury.

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

CAS No. : 126054-77-1

Size Price Stock Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
In-stock
Solution
10 mM * 1 mL in DMSO In-stock
Solid
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Customer Review

Based on 3 publication(s) in Google Scholar

Top Publications Citing Use of Products
Cell Proliferation/Viability Assay
IF
WB
Histological Imaging/Staining
Flow Cytometry

    Atractyloside A purchased from MedChemExpress. Usage Cited in: Front Microbiol. 2023 Jan 10:13:1067725.  [Abstract]

    Cell viability of Atractyloside A (1, 5, 10, 20, 30, 40, 50, 80, 100 μM) on A549 and MDCK.

    Atractyloside A purchased from MedChemExpress. Usage Cited in: Front Microbiol. 2023 Jan 10:13:1067725.  [Abstract]

    Immunofluorescence analysis of the expression of IBV nucleoprotein after infection treated with various concentrations of Atractyloside A (AA) for 24 h.

    Atractyloside A purchased from MedChemExpress. Usage Cited in: Front Microbiol. 2023 Jan 10:13:1067725.  [Abstract]

    Western blot analysis of RIG-I pathway proteins after IBV infection in Atractyloside A (20, 30, 40 μM) treatment groups with different drug concentrations.

    Atractyloside A purchased from MedChemExpress. Usage Cited in: Front Microbiol. 2023 Jan 10:13:1067725.  [Abstract]

    H&E analysis of lung tissue after infection treated with Atractyloside A (AA) (10, 30 mg/kg, p.o.).

    Atractyloside A purchased from MedChemExpress. Usage Cited in: Front Microbiol. 2023 Jan 10:13:1067725.  [Abstract]

    Effect of Atractyloside A treatment on the polarization levels of macrophages in vitro. Flow cytometry was performed to analyze the proportions of bone marrow-derived macrophages (BMMs).

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    Description

    Atractyloside A is an orally active inhibitor of the TLR4/MyD88/NF-κB signaling pathway and also an opener of the mitochondrial permeability transition pore (MPTP). Atractyloside A interferes with the activation of the TLR4/MyD88/NF-κB pathway, thereby inhibiting intestinal inflammatory responses. Atractyloside A reverses mucin synthesis impairment, improves intestinal barrier integrity, and restores homeostasis by altering the composition of the gut microbiota. Atractyloside A can be used in studies related to spleen deficiency diarrhea and myocardial injury[1][2].

    In Vitro

    Atractyloside A (10 μM; 12 h) abolishes the TRAP1-mediated protective effects on H9C2 cells in acidic medium (pH 6.5) by increasing MPTP opening, promoting apoptosis, reducing cell viability, impairing mitochondrial function, and disrupting mitochondrial ultrastructure[1].

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

    In Vivo

    Atractyloside-A (5-10 mg/kg; p.o.; daily; for 7 consecutive days) exerts a dose-dependent therapeutic effect on spleen-deficiency diarrhea (SDD) in male ICR mice[2].
    Atractyloside-A (10 mg/kg; p.o.; once daily; for 7 consecutive days) fails to alleviate SDD symptoms in male ICR mice with depleted gut microbiota, indicating that gut microbiota is essential for its therapeutic activity[2].

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

    Animal Model: ICR mice (male, 3 weeks old)[2]
    Dosage: 5 mg/kg; 10 mg/kg
    Administration: p.o.; daily; 7 days
    Result: Increased body weight gain compared to SDD mice; reduced fecal moisture, diarrhea scores, and diarrhea index; partially restored colon morphological structure, reduced colonic inflammatory cell infiltration, and increased goblet cell and MUC2 levels; upregulated colon AQP3, AQP4, and AQP8 expression; increased colonic ZO-1 and occludin tight junction protein levels; downregulated colonic pro-inflammatory cytokines TNF-α, IL-1β, IL-6, and serum DAO and 5-HT levels; upregulated colonic anti-inflammatory cytokine IL-10 levels; downregulated colonic TLR4, MyD88, p-IKK-α, p-IκB-α, and p-p65 protein expression; shifted intestinal flora composition toward the control group, including increased Lactobacillus abundance.
    Produced greater improvements than the 5 mg/kg dose, including significantly higher body weight gain from day 2 onward; significantly reduced fecal moisture, diarrhea scores, and diarrhea index; significantly increased colon length (exceeding control levels); fully restored colon morphological structure with reduced inflammation, increased goblet cell and MUC2 levels; significantly upregulated colon AQP3, AQP4, and AQP8 expression; significantly increased colonic ZO-1 and occludin levels; significantly downregulated colonic TNF-α, IL-1β, IL-6, serum DAO, and 5-HT levels; significantly upregulated colonic IL-10 levels; significantly downregulated colonic TNF-α, TLR4, MyD88, p-IKK-α, p-IκB-α, and p-p65 protein expression; normalized intestinal flora clustering to match the control group, with significant increases in Lactobacillus, Bacteroides, Ruminococcus, and Intestinimonas abundances.
    Molecular Weight

    448.50

    Formula

    C21H36O10

    CAS No.
    Appearance

    Solid

    Color

    White to light yellow

    SMILES

    O=C1[C@@](C)(O)[C@]2([H])C[C@H](C(C)(O[C@H]3[C@@H]([C@H]([C@@H]([C@@H](CO)O3)O)O)O)C)CC[C@@](CO)(O)[C@@]2([H])C1

    Structure Classification
    Initial Source
    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 : 50 mg/mL (111.48 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 2.2297 mL 11.1483 mL 22.2965 mL
    5 mM 0.4459 mL 2.2297 mL 4.4593 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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    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: ≥ 2.08 mg/mL (4.64 mM); Clear solution

      This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 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: ≥ 2.08 mg/mL (4.64 mM); Clear solution

      This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 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
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    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.
    Purity & Documentation

    Purity: 98.11%

    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 2.2297 mL 11.1483 mL 22.2965 mL 55.7414 mL
    5 mM 0.4459 mL 2.2297 mL 4.4593 mL 11.1483 mL
    10 mM 0.2230 mL 1.1148 mL 2.2297 mL 5.5741 mL
    15 mM 0.1486 mL 0.7432 mL 1.4864 mL 3.7161 mL
    20 mM 0.1115 mL 0.5574 mL 1.1148 mL 2.7871 mL
    25 mM 0.0892 mL 0.4459 mL 0.8919 mL 2.2297 mL
    30 mM 0.0743 mL 0.3716 mL 0.7432 mL 1.8580 mL
    40 mM 0.0557 mL 0.2787 mL 0.5574 mL 1.3935 mL
    50 mM 0.0446 mL 0.2230 mL 0.4459 mL 1.1148 mL
    60 mM 0.0372 mL 0.1858 mL 0.3716 mL 0.9290 mL
    80 mM 0.0279 mL 0.1394 mL 0.2787 mL 0.6968 mL
    100 mM 0.0223 mL 0.1115 mL 0.2230 mL 0.5574 mL
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      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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