| Size | Price | Stock | Qty |
|---|---|---|---|
| 1mg |
|
||
| 5mg |
|
||
| 10mg | |||
| Other Sizes |
| Targets |
Risarestat targets aldose reductase, the first and rate-limiting enzyme in the polyol pathway. It acts as an inhibitor of this enzyme. By inhibiting aldose reductase, risarestat prevents the conversion of glucose to sorbitol and subsequently to dulcitol (a polyol). This prevents the accumulation of polyols in tissues, which is implicated in the pathogenesis of diabetic complications.
|
|---|---|
| ln Vitro |
In vitro, risarestat is an aldose reductase inhibitor. It inhibits the accumulation of dulcitol in a dose-dependent manner. Its activity is assessed using enzyme assays with purified aldose reductase or in tissue culture models. These assays measure the reduction in sorbitol or dulcitol production.
|
| ln Vivo |
With the exception of the 1.0% solution, which exhibits activity similar to the 0.25% solution, rimarestat reduces the accumulation of dulcitol in a dose-dependent manner[1]. Within 30 minutes of injection, risarestat reaches its peak in the corneal epithelium, stroma, endothelium, and aqueous humor. Over the course of the next 24 hours, it progressively decreases in response to time. Up to 24 hours following injection, risarestat can be detected in the lens, with a peak concentration occurring two hours later[2]. The group treated with Risarestat showed a considerable decrease in the anterior surface area of superficial cells, with a mean value of 881 microns2 down to 728 microns2. From 5.36 to 1.37 g/mm2, there is a notable improvement in corneal sensitivity[3]. By the end of the seven-month trial, animals treated with Risarestat had a mean blink response that was considerably higher than that of untreated galactose-fed rats, but they did not differ significantly from controls. Within three weeks, rats fed galactose without treatment and those given Risarestat topically both acquire bilateral nuclear cataracts[4].
In vivo, risarestat has been developed for the treatment of diabetic complications. It has been studied for its effects on diabetic keratopathy and corneal epithelial disorders. Its clinical efficacy has been evaluated in studies. However, specific details of in vivo efficacy studies are not extensively detailed in the available literature. |
| Enzyme Assay |
The in vitro enzyme assay for risarestat measures its ability to inhibit aldose reductase activity. These cell-free assays use purified aldose reductase and a substrate such as DL-glyceraldehyde or glucose. The compound's inhibitory potency (IC50) is determined by measuring the reduction in enzyme activity. These assays confirm its mechanism as an aldose reductase inhibitor.
|
| Cell Assay |
In vitro cellular assays for risarestat assess its effects on polyol accumulation. Cells or tissues are cultured in high-glucose conditions in the presence of risarestat, and the accumulation of sorbitol or dulcitol is measured. These assays demonstrate the compound's ability to prevent polyol accumulation in a relevant cellular context.
|
| Animal Protocol |
In vivo animal studies for risarestat have been conducted in animal models of diabetes to evaluate its efficacy in preventing diabetic complications. However, specific details of these studies are not extensively detailed in the available literature. It is a research compound and is not approved for clinical use.
|
| ADME/Pharmacokinetics |
Specific pharmacokinetic data for risarestat are not extensively detailed in the available literature. As a small molecule, its pharmacokinetic properties would be important for its in vivo efficacy. However, specific parameters such as half-life and bioavailability are not provided. It is intended for research use only.
|
| Toxicity/Toxicokinetics |
Specific toxicity data for risarestat are not extensively detailed in the available literature. As an aldose reductase inhibitor, its toxicity profile is likely related to its mechanism of action. However, its potential for treating diabetic complications suggests a manageable safety profile. It is intended for research purposes only.
|
| References |
|
| Additional Infomation |
Risarestat is a thiazolidinone drug.
Risarestat (CT-112) is a thiazolidinedione-class aldose reductase inhibitor. It was developed for the treatment of diabetic complications, particularly diabetic keratopathy. It inhibits dulcitol accumulation in a dose-dependent manner. It is a research compound and is not approved for clinical use. |
| Molecular Formula |
C16H21NO4S
|
|---|---|
| Molecular Weight |
323.407
|
| Exact Mass |
323.119
|
| CAS # |
79714-31-1
|
| PubChem CID |
133264
|
| Appearance |
White to light yellow solid powder
|
| LogP |
4.007
|
| Hydrogen Bond Donor Count |
1
|
| Hydrogen Bond Acceptor Count |
5
|
| Rotatable Bond Count |
8
|
| Heavy Atom Count |
22
|
| Complexity |
390
|
| Defined Atom Stereocenter Count |
0
|
| InChi Key |
CRPGRUONUFDYBG-UHFFFAOYSA-N
|
| InChi Code |
InChI=1S/C16H21NO4S/c1-3-5-6-9-21-12-8-7-11(10-13(12)20-4-2)14-15(18)17-16(19)22-14/h7-8,10,14H,3-6,9H2,1-2H3,(H,17,18,19)
|
| Chemical Name |
2,4-Thiazolidinedione, 5-(3-ethoxy-4-(pentyloxy)phenyl)-
|
| Synonyms |
CT112 CT-112 Risarestat CT 112
|
| HS Tariff Code |
2934.99.9001
|
| 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)
|
| Solubility (In Vitro) |
DMSO : ~105 mg/mL (~324.67 mM)
|
|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 5.25 mg/mL (16.23 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 52.5 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 | 3.0921 mL | 15.4603 mL | 30.9205 mL | |
| 5 mM | 0.6184 mL | 3.0921 mL | 6.1841 mL | |
| 10 mM | 0.3092 mL | 1.5460 mL | 3.0921 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.
Products are for research use only; We do not sell to patients
Copyright 2020 InvivoChem LLC | All Rights Reserved
