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| 5mg |
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| 10mg |
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| 25mg |
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| Targets |
Imirestat targets aldose reductase (AKR1B1), the first enzyme in the polyol pathway. In normoglycemic states, this pathway plays a minor role in glucose metabolism. However, under hyperglycemic conditions, aldose reductase converts excess glucose to sorbitol, which can accumulate and cause cellular damage. By inhibiting aldose reductase, Imirestat prevents the accumulation of sorbitol and reduces diabetic complications.
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| ln Vitro |
Imirestat is a potent inhibitor of aldose reductase with IC50 values of 24 nM for the rat enzyme and 18 nM for the human enzyme. Its activity has been confirmed in various in vitro and in vivo studies. As an aldose reductase inhibitor, it blocks the polyol pathway and reduces the accumulation of sorbitol. It is a potent and specific inhibitor of AKR1B1.
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| ln Vivo |
Imirestat (1 mg/kg) enhances nerve conduction velocity without changing resistance to hypoxic conduction blocking or deficiencies in insulin-stimulated Oubain-sensitive ATPase activity [1].
Imirestat reduces periodontal bone loss in a rat model of P. gingivalis LPS-induced periodontal inflammation and bone reabsorption. It was developed to manage diabetic complications by blocking the polyol pathway. Its effects on diabetic neuropathy, retinopathy, and other metabolic disorders are being explored. |
| Enzyme Assay |
The primary in vitro assay for Imirestat is an aldose reductase enzyme activity assay using purified rat or human aldose reductase. The enzyme is incubated with its substrate, glucose, and the cofactor NADPH. The production of sorbitol or the oxidation of NADPH is measured spectrophotometrically in the presence of the compound. The IC50 values are determined from dose-response curves.
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| Cell Assay |
In vitro cellular experiments for Imirestat involve treating cells with the compound and measuring its effects on aldose reductase activity and sorbitol accumulation. Cells are cultured under high glucose conditions to simulate diabetic hyperglycemia. The accumulation of sorbitol is measured using enzymatic or chromatographic methods. The compound's effects on cellular damage and viability are also assessed.
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| Animal Protocol |
In vivo animal experiments for Imirestat have been conducted in a rat model of P. gingivalis LPS-induced periodontal inflammation and bone reabsorption, where it reduced periodontal bone loss. It could also be evaluated in animal models of diabetic neuropathy, retinopathy, and nephropathy to assess its efficacy in preventing or treating these complications.
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| ADME/Pharmacokinetics |
Imirestat has a molecular weight of 286.23 and a molecular formula of C15H8F2N2O2. It is also known as AL-1576. The compound is an aldose reductase inhibitor used for the treatment of diabetes. It has a purity of 95%. It is typically used as a research reagent.
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| Toxicity/Toxicokinetics |
Imirestat is a research compound that is not intended for human use. Its toxicological profile is not extensively characterized in the available literature. As with all research chemicals, standard safety precautions should be followed when handling. Its safety would need to be established for therapeutic applications.
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| References | |
| Additional Infomation |
Imirestat (AL-1576) is a potent and specific inhibitor of aldose reductase (AKR1B1) with IC50 values of 24 nM for the rat enzyme and 18 nM for the human enzyme. It blocks the polyol pathway and reduces the accumulation of sorbitol. Imirestat is used in research exploring treatments for diabetic complications.
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| Molecular Formula |
C15H8F2N2O2
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|---|---|
| Molecular Weight |
286.2378
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| Exact Mass |
286.055
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| CAS # |
89391-50-4
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| PubChem CID |
65673
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| Appearance |
White to off-white solid powder
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| Density |
1.58g/cm3
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| Index of Refraction |
1.692
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| LogP |
2.685
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| Hydrogen Bond Donor Count |
2
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| Hydrogen Bond Acceptor Count |
4
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| Rotatable Bond Count |
0
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| Heavy Atom Count |
21
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| Complexity |
472
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| Defined Atom Stereocenter Count |
0
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| InChi Key |
QCCHBHSAIQIQGO-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C15H8F2N2O2/c16-7-1-3-9-10-4-2-8(17)6-12(10)15(11(9)5-7)13(20)18-14(21)19-15/h1-6H,(H2,18,19,20,21)
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| Chemical Name |
2,7-difluorospiro[fluorene-9,5'-imidazolidine]-2',4'-dione
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| Synonyms |
AL-01576 AL-1576 ImirestatAL01576AL1576 Hoe-843
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO : ~83.33 mg/mL (~291.13 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.08 mg/mL (7.27 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.08 mg/mL (7.27 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 3.4936 mL | 17.4679 mL | 34.9357 mL | |
| 5 mM | 0.6987 mL | 3.4936 mL | 6.9871 mL | |
| 10 mM | 0.3494 mL | 1.7468 mL | 3.4936 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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