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.

Epalrestat Chemical Structure

Epalrestat Chemical Structure

CAS No. : 82159-09-9

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10 mM * 1 mL in DMSO
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Customer Review

Based on 2 publication(s) in Google Scholar

Other Forms of Epalrestat:

Epalrestat Related Antibodies

Top Publications Citing Use of Products

  • 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)

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Molecular Weight *

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

This equation is commonly abbreviated as: C1V1 = C2V2

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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: 99.72%

COA (248 KB) HNMR (256 KB) LCMS (270 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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