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Epalrestat [82159-09-9]

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Referentie NB-64-05996-1mL

Formaat : 1mLx10mM(inDMSO)

Merk : Neo Biotech

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Epalrestat

(Synonyms: ONO2235) Copy Product Info

Synonyms: ONO2235

Catalog No. T1458 Copy Product Info

Purity: 99.66%

Epalrestat (ONO2235), an aldose reductase inhibitor, is well tolerated in Long-term therapy. It can effectually ameliorate the associated symptoms of diabetic neuropathy and delay the progression of the disease, particularly in patients with limited microangiopathy and good glycemic control.

Cas No. 82159-09-9

For research use only—not for human use. No sales to individuals. Use as intended only.

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Purity:99.66%

Appearance:Solid

Product Information

Epalrestat AI Summary

Epalrestat exhibits potent inhibitory activity against rat lens aldose reductase (ALR2) with an IC50 value ranging from 10.0 to 72.0 nM in various assays. It also shows inhibitory activity against pig kidney aldehyde reductase (ALR1) with selectivity ratios up to 1500 nM, and human aldose reductase enzymes with IC50 values as potent as 21.0 nM. In addition, it demonstrates selective inhibition, with a lower IC50 for ALR2 compared to ALR1, highlighting its potential therapeutic applications in conditions requiring aldose reductase inhibition. Epalrestat has shown permeability in Wistar rat jejunum, suggesting good oral bioavailability, and exhibits antioxidant properties and cytoprotective activities in hyperglycemic conditions. It also indicates some level of hepatotoxicity but does not inhibit advanced glycation end-product formation. Additionally, Epalrestat demonstrates moderate antiviral activity against SARS-CoV-2, shown by its inhibition of virus-induced cytotoxicity in cell assays..

Note: Summary generated by AI. Data source: ChEMBL

Bioactivity

Description	Epalrestat (ONO2235), an aldose reductase inhibitor, is well tolerated in Long-term therapy. It can effectually ameliorate the associated symptoms of diabetic neuropathy and delay the progression of the disease, particularly in patients with limited microangiopathy and good glycemic control.
Synonyms	ONO2235

Chemical Properties

Molecular Weight	319.4
Formula	C₁₅H₁₃NO₃S₂
Cas No.	82159-09-9
Smiles	CC(=C/C1=CC=CC=C1)\C=C1/SC(=S)N(CC(O)=O)C1=O
Relative Density.	1.43 g/cm3

Storage & Solubility Information

Storage

Keep away from direct sunlight,Keep away from moisture, Powder: -20°C for 3 years | In solvent: -80°C for 1 year Shipping with blue ice/Shipping at ambient temperature.

Solubility Information

DMSO: 23.18 mg/mL (72.57 mM), Sonication is recommended.

In Vivo Formulation

10% DMSO+90% Corn Oil: 0.5 mg/mL (1.57 mM), Sonication is recommended.

Please add the solvents sequentially, clarifying the solution as much as possible before adding the next one. Dissolve by heating and/or sonication if necessary. Working solution is recommended to be prepared and used immediately. The formulation provided above is for reference purposes only. In vivo formulations may vary and should be modified based on specific experimental conditions.

Solution Preparation Table

DMSO

	1mg	5mg	10mg	50mg
1 mM	3.1309 mL	15.6544 mL	31.3087 mL	156.5435 mL
5 mM	0.6262 mL	3.1309 mL	6.2617 mL	31.3087 mL
10 mM	0.3131 mL	1.5654 mL	3.1309 mL	15.6544 mL
20 mM	0.1565 mL	0.7827 mL	1.5654 mL	7.8272 mL
50 mM	0.0626 mL	0.3131 mL	0.6262 mL	3.1309 mL

Note : The dilution table applies only to solid products. For liquid products, please calculate the stock solution based on the stated concentration and/or density.

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In Vivo Formulation Calculator (Clear solution)

Please enter your animal experiment information in the following box and click Calculate to obtain the stock solution preparation method and in vivo formula preparation method:

For example, if the intended dosage is 10 mg/kg for animals weighing 20 g , with a dosing volume of 100 μL per animal, and a total of 10 animals are to be administered, using a formulation of 10% DMSO+ 40% PEG300+ 5% Tween 80+ 45% Saline/PBS/ddH₂O , the resulting working solution concentration would be 2 mg/mL.

Stock Solution Preparation:

Dissolve 2 mg of the compound in 100 μL DMSO to obtain a stock solution at a concentration of 20 mg/mL . If the required concentration exceeds the compound's known solubility, please contact us for technical support before proceeding.

Preparation of the In Vivo Formulation:

1) Add 100 μL of the DMSO stock solution to 400 µL PEG300 and mix thoroughly until the solution becomes clear.

2) Add 50 µL Tween 80 and mix well until fully clarified.

3) Add 450 µL Saline,PBS or ddH₂O and mix thoroughly until a homogeneous solution is obtained.

This example is provided solely to demonstrate the use of the In Vivo Formulation Calculator and does not constitute a recommended formulation for any specific compound. Please select an appropriate dissolution and formulation strategy based on your experimental model and route of administration.

All co-solvents required for this protocol, includingDMSO, PEG300/PEG400, Tween 80, SBE-β-CD, and Corn oil, are available for purchase on the TargetMol website.

Dose Conversion

Please see Product Handling Instructions for more frequently ask questions. Topics include: how to prepare stock soluti