Art. -Nr.: HY-66009

Epalrestat

Name: Epalrestat
Brand: MedChemExpress
SKU: HY-66009
Price: 35.00 USD
Availability: InStock
Rating: 5 (10 reviews)

(Synonyms: ONO2235)

10 Cited Publications

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Based on 10 publication(s) in Google Scholar

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

Nur für Forschungszwecke. Wir verkaufen nicht an Patienten.

Reinheit : 99.62%
CAS. Nr.: 82159-09-9
Formel: C₁₅H₁₃NO₃S₂
Molecular Weight:319.40

Speicherung:

-20°C, protect from light

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

Epalrestat Chemical Structure

CAS. Nr.: 82159-09-9

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Biologische Aktivität
- Beschreibung
- In Vitro
- In Vivo
Chemical Information
Publications (10)
Lösungsmittel & Löslichkeit
- In Vitro
- In Vivo
Reinheit & Dokumentation
Verweise
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

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.

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.

Chemical Information

CAS. Nr. 82159-09-9
Appearance Solid
Molecular Weight 319.40
Formel C₁₅H₁₃NO₃S₂
Color Pink to red
SMILES

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

ONO2235
Versand

Room temperature in continental US; may vary elsewhere.
Speicherung

-20°C, protect from light

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

Publications (10)

All Cell Proliferation/Viability AssayWBELISAFlow CytometryHistological Imaging/Staining

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Journal Impact Factor

J Transl Med

Novel role for epalrestat: protecting against NLRP3 inflammasome-driven NASH by targeting aldose reductase. [Abstract]

2023 Oct 7;21(1):700. PMID: 37805545

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.
Dev Cell

SMARCA5 reprograms AKR1B1-mediated fructose metabolism to control leukemogenesis. [Abstract]

2024 Aug 5;59(15):1954-1971.e7. PMID: 38776924
Int J Biol Macromol

Targeting aldose reductase in pulmonary fibrosis: Blocking de novo fatty acid synthesis halts pro-fibrotic M2 polarization. [Abstract]

2025 Dec 9:149590. PMID: 41380895
Clin Transl Med

2026 Sep;16(9):e70796. PMID: 42707018
Cell Mol Life Sci

Glycosphingolipid synthesis is impaired in SLC35A2-CDG and improves with galactose supplementation. [Abstract]

2025 Jun 27;82(1):257. PMID: 40576648
Cell Mol Life Sci

2025 Jun 27;82(1):257.
Bioorg Med Chem

Inhibition of LPS-induced inflammatory response in RAW264.7 cells by natural Chlorogenic acid isomers involved with AKR1B1 inhibition. [Abstract]

2024 Nov 15:114:117942. PMID: 39396466
Hepat Med

Aldose Reductase Mediated Mitophagy Promotes Epithelial-Mesenchymal Transition of Hepatocytes. [Abstract]

2025 Oct 1:17:141-159. PMID: 41054599
NPJ Metab Health Dis

2026 Jul 1;4(1):24. PMID: 42386885
Res Sq

2026 Jun 11.

Lösungsmittel & Löslichkeit

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)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

3.1309 mL

15.6544 mL

31.3087 mL

5 mM

0.6262 mL

3.1309 mL

6.2617 mL

10 mM

0.3131 mL

1.5654 mL

3.1309 mL

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.

Molaritätsrechner

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

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

Stock Solution Working Solution

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.

Working Solution

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 Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
Saline +

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).

Working solution concentration: 0.22 mg/mL

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (281 KB)
SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

Verweise

[1]. Ramirez, M.A. and N.L. Borja, Epalrestat: an aldose reductase inhibitor for the treatment of diabetic neuropathy. Pharmacotherapy, 2008. 28(5): p. 646-55. [Content Brief]

[2]. Okamoto, H., et al., Effects of epalrestat, an aldose reductase inhibitor, on diabetic neuropathy and gastroparesis. Intern Med, 2003. 42(8): p. 655-64. [Content Brief]

[3]. Hotta, N., et al., Clinical investigation of epalrestat, an aldose reductase inhibitor, on diabetic neuropathy in Japan: multicenter study. Diabetic Neuropathy Study Group in Japan. J Diabetes Complications, 1996. 10(3): p. 168-72. [Content Brief]

[4]. He J, et al. The aldose reductase inhibitor epalrestat exerts nephritic protection on diabetic nephropathy in db/db mice through metabolic modulation. Acta Pharmacol Sin. 2019 Jan;40(1):86-97. [Content Brief]

[5]. Sato K, et al. Epalrestat increases intracellular glutathione levels in Schwann cells through transcription regulation. Redox Biol. 2013 Nov 19;2:15-21. [Content Brief]

[6]. Li QR, et al. Epalrestat protects against diabetic peripheral neuropathy by alleviating oxidative stress and inhibiting polyol pathway. Neural Regen Res. 2016 Feb;11(2):345-51. [Content Brief]

[7]. Zhang T, et al. The Aldose Reductase Inhibitor Epalrestat Maintains Blood-Brain Barrier Integrity by Enhancing Endothelial Cell Function during Cerebral Ischemia. Mol Neurobiol. 2023 Jul;60(7):3741-3757. [Content Brief]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

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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Keywords

Epalrestat

10 Cited Publications

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Epalrestat

Publications Citing Use of MedChemExpress (MCE) Epalrestat