| Size | Price | Stock | Qty |
|---|---|---|---|
| 10mg |
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| 25mg |
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| 50mg |
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| 100mg |
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| 250mg |
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| 500mg |
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| Other Sizes |
Purity: ≥98%
| Targets |
Aldose reductase (rat lens enzyme). Alrestatin selectively inhibits aldose reductase with an IC50 of 1.5 µM for the rat lens enzyme. It shows selectivity for rat lens aldose reductase over rat kidney aldehyde reductase (IC50 = 58 µM). Inhibition of aldose reductase prevents the accumulation of sorbitol in tissues, which is implicated in diabetic complications.
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| ln Vitro |
Alrestatin inhibits aldose reductase in vitro with an IC50 of 1.5 µM for the rat lens enzyme. It is selective for aldose reductase over aldehyde reductase (IC50 = 58 µM). The compound attenuates glucose-induced angiotensin II production in rat vascular smooth muscle in vitro. It also inhibits gastric acid secretion.
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| ln Vivo |
In vivo, Alrestatin has been studied for its potential to prevent diabetic complications such as neuropathy and retinopathy. It inhibits gastric acid secretion and decreases the volume of gastric juice in pylorus-ligated rats. The compound has been used in pharmacological research to study the role of aldose reductase in polyol pathway activation.
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| Enzyme Assay |
In vitro enzyme inhibition assays for Alrestatin involve measuring aldose reductase activity in the presence of varying concentrations of the compound. The enzyme is typically purified from rat lens. Activity is measured by monitoring the reduction of DL-glyceraldehyde or glucose to sorbitol in the presence of NADPH. The IC50 is determined from dose-response curves. Selectivity is assessed by comparing activity against aldehyde reductase.
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| Cell Assay |
Cellular assays for Alrestatin are not extensively documented. When performed, they typically involve vascular smooth muscle cells cultured in high glucose conditions. Cells are treated with Alrestatin, and angiotensin II production is measured. The compound's ability to attenuate glucose-induced effects is assessed.
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| Animal Protocol |
In vivo animal studies for Alrestatin have been conducted in rat models. The compound is typically administered orally or intraperitoneally. Gastric acid secretion is measured in pylorus-ligated rats. Effects on diabetic complications may be assessed in streptozotocin-induced diabetic models by measuring nerve conduction velocity, lens opacity, or renal function. Dosing regimens vary.
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| ADME/Pharmacokinetics |
Pharmacokinetic data for Alrestatin are limited. The compound has a molecular weight of 255.23 and a molecular formula of C14H9NO4. It is typically stored at room temperature. The compound is soluble in DMSO. Detailed ADME parameters are not extensively documented. It is intended for research use only.
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| Toxicity/Toxicokinetics |
Toxicological data for Alrestatin are limited. The compound is a research chemical and is not approved for human therapeutic use. Standard laboratory safety precautions should be taken when handling the compound. It should be stored under recommended conditions. No specific toxicity data are available in publicly accessible sources.
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| References |
Gabbay KH, Spack N, Loo S, Hirsch HJ, Ackil AA. Aldose reductase inhibition: studies with alrestatin. Metabolism. 1979 Apr;28(4 Suppl 1):471-6. PubMed PMID: 122298.
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| Additional Infomation |
Alrestatin (AY-22284) is a first-generation aldose reductase inhibitor with an IC50 of 1.5 µM for the rat lens enzyme. It is selective for aldose reductase over aldehyde reductase. The compound has been studied for its potential to prevent diabetic complications. It is not approved for clinical use and is available for research purposes only. Its molecular formula is C14H9NO4.
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| Molecular Formula |
C14H9NO4
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|---|---|
| Molecular Weight |
255.229
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| Exact Mass |
167.982
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| CAS # |
51411-04-2
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| Related CAS # |
Alrestatin sodium;51876-97-2
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| PubChem CID |
2120
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| Appearance |
White to off-white solid powder
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| Density |
1.7±0.1 g/cm3
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| Boiling Point |
359.1±44.0 °C at 760 mmHg
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| Flash Point |
171.0±28.4 °C
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| Vapour Pressure |
0.0±1.7 mmHg at 25°C
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| Index of Refraction |
1.480
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| LogP |
-2.47
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
4
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| Rotatable Bond Count |
2
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| Heavy Atom Count |
19
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| Complexity |
403
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| Defined Atom Stereocenter Count |
0
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| InChi Key |
1,3-Dioxo-1H-benz(de)isoquinoline-2(3H)-acetic acid
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| InChi Code |
GCUCIFQCGJIRNT-UHFFFAOYSA-N
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| Chemical Name |
1,3-Dioxo-1H-benz(de)isoquinoline-2(3H)-acetic acid
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| Synonyms |
Alrestatin AY-22284 AY 22284 AY22284 Alrestatin free acid
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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 : ~50 mg/mL (~195.90 mM)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (9.80 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 25.0 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: 2.5 mg/mL (9.80 mM) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), suspension solution; with ultrasonication. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.5 mg/mL (9.80 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 3.9180 mL | 19.5902 mL | 39.1803 mL | |
| 5 mM | 0.7836 mL | 3.9180 mL | 7.8361 mL | |
| 10 mM | 0.3918 mL | 1.9590 mL | 3.9180 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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