2. Metabolic Enzyme/Protease
  3. Aldose Reductase
  4. Epalrestat

Epalrestat is an orally active aldose reductase inhibitor that acts on diabetic neuropathy.

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

CAS No. : 82159-09-9

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Customer Review

Based on 6 publication(s) in Google Scholar

Other Forms of Epalrestat:

Epalrestat Related Antibodies

Top Publications Citing Use of Products

    Epalrestat purchased from MedChemExpress. Usage Cited in: J Transl Med. 2023 Oct 7;21(1):700.  [Abstract]

    Cell viability of BMDMs treated with Epalrestat (2.5-200 μM) for 24 h as detected using a CCK-8 reagent.

    Epalrestat purchased from MedChemExpress. Usage Cited in: J Transl Med. 2023 Oct 7;21(1):700.  [Abstract]

    LPS-primed BMDMs were treated with various doses of Epalrestat (10, 20, 40 μM) for 1 h before stimulation with nigericin for 30 min. Immunoblot analysis of epalrestat was used to detect cleaved caspase-1 and IL-1β in the cell supernatants (Sup.) and the expression of NLRP3, caspase-1 p45, pro-IL-1β, and ASC in the cell lysates (Lys.).

    Epalrestat purchased from MedChemExpress. Usage Cited in: J Transl Med. 2023 Oct 7;21(1):700.  [Abstract]

    Epalrestat (10, 20, 40 μM) significantly inhibited the production of IL-1β by ELISA.

    Epalrestat purchased from MedChemExpress. Usage Cited in: J Transl Med. 2023 Oct 7;21(1):700.  [Abstract]

    Mice were intraperitoneally injected with LPS or PBS for 6 h after pre-treatment with Epalrestat or vehicle. Peritoneal macrophages pre-treated with Epalrestat (20, 40 mg/kg, i.g.) could also be decrease, as measured via flow cytometry.

    Epalrestat purchased from MedChemExpress. Usage Cited in: J Transl Med. 2023 Oct 7;21(1):700.  [Abstract]

    These pathological changes were significantly reduced after Epalrestat (20 mg/kg, i.g.) treatment stained with H&E, Masson stain, and Sirius red.

    • Biological Activity

    • Purity & Documentation

    • References

    • Customer Review

    Description

    Epalrestat is an orally active aldose reductase inhibitor that acts on diabetic neuropathy[1][2][3].

    In Vitro

    Epalrestat (100 and 200 µM, 24 h) inhibits cell viability and induces cell apoptosis in rat Schwann cells (SCs)[5].
    Epalrestat (10 and 50 µM, 24 h) increases intracellular glutathione levels in rat SCs by up-regulating γ-GCS via Nrf2 activation[5].
    Epalrestat (50 µM, 16 h) protects SCs from oxidative stress[5].

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

    Epalrestat Related Antibodies

    RT-PCR[5]

    Cell Line: rat SCs
    Concentration: 10 or 50 µM
    Incubation Time: 4 h
    Result: Increased the nuclear level of active Nrf2 by 1.8- and 3.8-fold at 10 and 50 µM, and failed to increase Nrf2 mRNA levels.
    In Vivo

    Epalrestat (0.08% (w/w) in regular chow, 8 weeks) shows nephritic protective effect in diabetic nephropathy in db/db mice[4].
    Epalrestat (100 mg/kg, i.g., daily for 6 weeks) protects rats from diabetic peripheral nerve injury in diabetic peripheral neuropathy (DPN) model induced by Streptozotocin (HY-13753)[6].
    Epalrestat (50 mg/kg, oral gavage, twice a day) reduces cerebral ischemia-induced infarct volume and BBB permeability in mice[7].

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

    Animal Model: db/db mice[4]
    Dosage: 0.08% (w/w) in fed regular chow
    Administration: 8 weeks
    Result: Ameliorated GBM thickening and mesangial matrix deposition in kidney tissue.
    Reduced the elevated sorbitol and fructose in the plasma, urine, and renal cortex of db/db mice.
    Reduced myo-inositol in the plasma and urine, whereas increased myo-inositol in the renal cortex.
    Animal Model: Rats were treated with high-fat and high-sugar diet for 4 weeks, and injected with Streptozotocin at 4 and 8 weeks[6]
    Dosage: 100 mg/kg/d
    Administration: i.g. 6 weeks
    Result: Improved pathological structures of neurites and myelin.
    Increased SOD, CAT and GPX protein levels in sciatic nerves.
    Decrease aldose reductase level in sciatic nerves.
    Clinical Trial
    Molecular Weight

    319.40

    Formula

    C15H13NO3S2
    CAS No.
    Appearance

    Solid

    Color

    Pink to red

    SMILES

    O=C(O)CN(C/1=O)C(SC1=C/C(C)=C/C2=CC=CC=C2)=S
    Shipping

    Room temperature in continental US; may vary elsewhere.
    Storage

    -20°C, protect from light

    *In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

    Solvent & Solubility
    In Vitro: 

    DMSO : 20 mg/mL (62.62 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 3.1309 mL 15.6544 mL 31.3087 mL
    5 mM 0.6262 mL 3.1309 mL 6.2617 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, 6 months; -20°C, 1 month (protect from light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

    • Molarity Calculator

    • Dilution Calculator

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

    Mass
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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    90% Corn Oil

      Solubility: ≥ 2 mg/mL (6.26 mM); Clear solution

      This protocol yields a clear solution of ≥ 2 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 (20.0 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:  0.5% CMC-Na/saline water

      Solubility: 10 mg/mL (31.31 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)

    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).

    *In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

    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: 99.62%

    SDS (393 KB)

    COA (248 KB) HNMR (259 KB) RP-HPLC (223 KB) MS (205 KB)

    Handling Instructions (2659 KB)
    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, 6 months; -20°C, 1 month (protect from light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

    Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
    DMSO 1 mM 3.1309 mL 15.6544 mL 31.3087 mL 78.2718 mL
    5 mM 0.6262 mL 3.1309 mL 6.2617 mL 15.6544 mL
    10 mM 0.3131 mL 1.5654 mL 3.1309 mL 7.8272 mL
    15 mM 0.2087 mL 1.0436 mL 2.0872 mL 5.2181 mL
    20 mM 0.1565 mL 0.7827 mL 1.5654 mL 3.9136 mL
    25 mM 0.1252 mL 0.6262 mL 1.2523 mL 3.1309 mL
    30 mM 0.1044 mL 0.5218 mL 1.0436 mL 2.6091 mL
    40 mM 0.0783 mL 0.3914 mL 0.7827 mL 1.9568 mL
    50 mM 0.0626 mL 0.3131 mL 0.6262 mL 1.5654 mL
    60 mM 0.0522 mL 0.2609 mL 0.5218 mL 1.3045 mL
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    Epalrestat 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:

    Epalrestat82159-09-9ONO2235ONO 2235ONO-2235Aldose ReductaseSCsoxidative stressdiabeticdb/db miceInhibitorinhibitorinhibit

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