| Size | Price | Stock | Qty |
|---|---|---|---|
| 5mg |
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| 10mg |
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| 500mg | |||
| 1g | |||
| Other Sizes |
| Targets |
Aldose reductase. Alrestatin Sodium selectively inhibits aldose reductase, the first enzyme in the polyol pathway that converts glucose to sorbitol. Inhibition of this enzyme prevents the accumulation of sorbitol in tissues, which is implicated in the pathogenesis of diabetic complications including neuropathy, retinopathy, and nephropathy.
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|---|---|
| ln Vitro |
Alrestatin Sodium is a specific inhibitor of aldose reductase in vitro. It inhibits the enzyme with potency comparable to Alrestatin free acid. The compound has been studied for its ability to prevent glucose-induced cellular damage in various in vitro models. It also inhibits gastric acid secretion.
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| ln Vivo |
In vivo, Alrestatin Sodium has been studied for its potential to prevent diabetic complications in animal models. It inhibits gastric acid secretion and decreases gastric juice volume in pylorus-ligated rats. The compound is structurally related to tolrestat, which was briefly marketed for diabetic complications.
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| Enzyme Assay |
In vitro enzyme inhibition assays for Alrestatin Sodium are similar to those for Alrestatin free acid. Aldose reductase activity is measured in the presence of varying concentrations of the compound. The enzyme is typically purified from rat lens. Activity is monitored by measuring the reduction of glucose to sorbitol in the presence of NADPH. IC50 values are determined from dose-response curves.
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| Cell Assay |
Cellular assays for Alrestatin Sodium are not extensively documented. When performed, they typically involve cells cultured in high glucose conditions to model diabetic complications. Cells are treated with Alrestatin Sodium, and markers of cellular damage or polyol pathway activity are measured.
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| Animal Protocol |
In vivo animal studies for Alrestatin Sodium have been conducted in rat models. The compound is typically administered orally or intraperitoneally. Effects on diabetic complications may be assessed in streptozotocin-induced diabetic models. Gastric acid secretion studies have also been performed in pylorus-ligated rats. Dosing regimens vary.
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| ADME/Pharmacokinetics |
Pharmacokinetic data for Alrestatin Sodium are limited. The compound has a molecular weight of 277.21 and a molecular formula of C14H8NNaO4. It is soluble in DMSO. The compound is intended for research use only. Detailed ADME parameters are not extensively documented.
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| Toxicity/Toxicokinetics |
Alrestatin Sodium is a research chemical and is not approved for human therapeutic use. It is structurally related to tolrestat, which was withdrawn from the market. Standard laboratory safety precautions should be taken when handling the compound. No specific toxicity data are available in publicly accessible sources.
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| References |
Aldose reductase inhibition: studies with alrestatin. Metabolism. 1979 Apr;28(4 Suppl 1):471-6.
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| Additional Infomation |
Alrestatin Sodium (AY-22284A) is the sodium salt of Alrestatin, a first-generation aldose reductase inhibitor. It inhibits aldose reductase, an enzyme involved in diabetic complications. The compound is structurally related to tolrestat. It is not approved for clinical use and is available for research purposes only. Its molecular formula is C14H8NNaO4.
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| Molecular Formula |
C14H8NNAO4
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|---|---|
| Molecular Weight |
277.21
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| Exact Mass |
277.035
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| CAS # |
51876-97-2
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| Related CAS # |
Alrestatin;51411-04-2
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| PubChem CID |
23683779
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| Appearance |
Typically exists as solid at room temperature
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| Density |
1.511g/cm3
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| Boiling Point |
512.7ºC at 760mmHg
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| Flash Point |
263.9ºC
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| Hydrogen Bond Donor Count |
0
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| Hydrogen Bond Acceptor Count |
4
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| Rotatable Bond Count |
2
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| Heavy Atom Count |
20
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| Complexity |
409
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| Defined Atom Stereocenter Count |
0
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| SMILES |
O=C([O-])CN(C(C1=CC=CC2=CC=CC3=C12)=O)C3=O.[Na+]
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| InChi Key |
FKZUETPACPDEAD-UHFFFAOYSA-M
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| InChi Code |
InChI=1S/C14H9NO4.Na/c16-11(17)7-15-13(18)9-5-1-3-8-4-2-6-10(12(8)9)14(15)19/h1-6H,7H2,(H,16,17)/q+1/p-1
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| Chemical Name |
Sodium 2-(1,3-Dioxobenzo[de]isoquinolin-2-yl)acetate
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| Synonyms |
Alrestatin Sodium AY22284A AY 22284A AY-22284A
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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) |
May dissolve in DMSO (in most cases), if not, try other solvents such as H2O, Ethanol, or DMF with a minute amount of products to avoid loss of samples
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| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 3.6074 mL | 18.0369 mL | 36.0737 mL | |
| 5 mM | 0.7215 mL | 3.6074 mL | 7.2147 mL | |
| 10 mM | 0.3607 mL | 1.8037 mL | 3.6074 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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