Lidorestat
Based on 1 Customer Validation
Lidorestat (IDD-676) is a potent, selective and orally active aldose reductase inhibitor with an IC50 of 5 nM. Lidorestat can be used for chronic diabetes complications. Lidorestat also improves nerve conduction and reduces cataract formation.
For research use only. We do not sell to patients.
- Purity: 99.50%
- CAS No.: 245116-90-9
- Formula: C18H11F3N2O2S
- Molecular Weight:376.35
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Storage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
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Biological Activity
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Chemical Information
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Solvent & Solubility
- Purity & Documentation
- References
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Help & FAQs
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Metabolism/Protease Compound Library
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Clinical Compound Library
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Drug Repurposing Compound Library
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Anti-diabetic Compound Library
HY-L040
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Glucose Metabolism Compound Library
HY-L092
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Heterocyclic Compound Library
HY-L138
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Metabolic Enzyme Compound Library
HY-L146
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Highly Selective Inhibitors Library
HY-L158
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Bioactive Compound Library Max
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Bioactive Compound Library
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High-Throughput Bioactive Compound Library
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Biological Activity
IC50: 5 nM (Rldose reductase)[1]
From in vitro experiments, Lidorestat has a reported IC50 against recombinant human aldose reductase (/h/-ALR2) of 5 μM. Against recombinant human aldehyde reductase (/h/-ALR1), Lidorestat has a reported IC50 of 27,000 μM, yielding a selectivity of /h/-ALR1//h/-ALR2 of 5400:1[1][2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Diabetic low-density lipoprotein (LDL) receptor-deficient [Ldlr(-/-)] mice[1]
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Dosage:25 mg/kg/day
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Administration:Oral administration; twice daily; for 6 weeks
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Result:Diabetic hAR-expressing mice had decreased fructose and reduced mortality.
| NCT Number | Sponsor | Condition | Start Date |
Phase
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|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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CAS No. 245116-90-9
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Appearance Solid
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Molecular Weight 376.35
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Formula C18H11F3N2O2S
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Color Light yellow to yellow
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SMILES
OC(CN1C(C=CC=C2)=C2C(CC3=NC(C(F)=C(F)C=C4F)=C4S3)=C1)=O
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Synonyms
IDD-676
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Solvent & Solubility
DMSO : 50 mg/mL (132.86 mM; ultrasonic and warming and heat to 60°C; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.08 mg/mL (5.53 mM); Clear solution
This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 0.56 mg/mL (1.49 mM); Clear solution
This protocol yields a clear solution of ≥ 0.56 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (5.6 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Purity & Documentation
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Data Sheet (273 KB)
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SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
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Handling Instructions (2659 KB)
References
[1]. Noh HL, et al. Regulation of plasma fructose and mortality in mice by the aldose reductase inhibitor lidorestat. J Pharmacol Exp Ther. 2009 Feb;328(2):496-503. [Content Brief]
[2]. Van Zandt MC, et al. Discovery of 3-[(4,5,7-trifluorobenzothiazol-2-yl)methyl]indole-N-acetic acid (lidorestat) and congeners as highly potent and selective inhibitors of aldose reductase for treatment of chronic diabetic complications. J Med Chem. 2005 May 5;48(9):3141-52. [Content Brief]
[3]. Maccari R, et al. Identification of new non-carboxylic acid containing inhibitors of aldose reductase. Bioorg Med Chem. 2010 Jun 1;18(11):4049-55. [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 2.6571 mL | 13.2855 mL | 26.5710 mL | 66.4275 mL |
| 5 mM | 0.5314 mL | 2.6571 mL | 5.3142 mL | 13.2855 mL | |
| 10 mM | 0.2657 mL | 1.3286 mL | 2.6571 mL | 6.6428 mL | |
| 15 mM | 0.1771 mL | 0.8857 mL | 1.7714 mL | 4.4285 mL | |
| 20 mM | 0.1329 mL | 0.6643 mL | 1.3286 mL | 3.3214 mL | |
| 25 mM | 0.1063 mL | 0.5314 mL | 1.0628 mL | 2.6571 mL | |
| 30 mM | 0.0886 mL | 0.4429 mL | 0.8857 mL | 2.2143 mL | |
| 40 mM | 0.0664 mL | 0.3321 mL | 0.6643 mL | 1.6607 mL | |
| 50 mM | 0.0531 mL | 0.2657 mL | 0.5314 mL | 1.3286 mL | |
| 60 mM | 0.0443 mL | 0.2214 mL | 0.4429 mL | 1.1071 mL | |
| 80 mM | 0.0332 mL | 0.1661 mL | 0.3321 mL | 0.8303 mL | |
| 100 mM | 0.0266 mL | 0.1329 mL | 0.2657 mL | 0.6643 mL |
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