Ponalrestat
Based on 1 publication(s) in Google Scholar
Ponalrestat (ICI 128436) is an orally active, selective and noncompetitive aldose reductase (AKR1B1; ALR) inhibitor. Ponalrestat selectively inhibits ALR2 (Ki=7.7 nM) over ALR1 (Ki=60 μM). Ponalrestat inhibits the conversion of glucose to sorbitol.
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- Pureza: 99.51%
- No. CAS: 72702-95-5
- Fòrmula: C17H12BrFN2O3
- Peso molecular:391.19
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Almacenamiento:
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
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Actividad biológica
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Chemical Information
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Solvente y solubilidad
- Pureza y Documentación
- Referencias
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Help & FAQs
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Metabolism/Protease Compound Library
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HY-L026
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HY-L092
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HY-L099
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HY-L146
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Publications Citing Use of MedChemExpress (MCE) Ponalrestat
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Actividad biológica
Ki: 7.7 nM (ALR2) and 60 μM (ALR1)[1]
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Adult female Sprague-Dawley rats[3]
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Dosage:10, 50 mg/kg
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Administration:Orally; daily; 8 weeks
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Result:Reduced sorbitol accumulation.
Chemical Information
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No. CAS 72702-95-5
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Appearance Solid
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Peso molecular 391.19
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Fòrmula C17H12BrFN2O3
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Color White to off-white
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SMILES
OC(CC(C1=C2C=CC=C1)=NN(CC3=C(C=C(Br)C=C3)F)C2=O)=O
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Synonyms
ICI 128436
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
Publications (1)
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Journal Impact Factor
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Most Recent
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J Transl Med
Novel role for epalrestat: protecting against NLRP3 inflammasome-driven NASH by targeting aldose reductase. [Abstract]2023 Oct 7;21(1):700. PMID: 37805545
Solvente y solubilidad
DMSO : 62.5 mg/mL (159.77 mM; Need ultrasonic; 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 (sealed storage, away from moisture). 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 (sealed storage, away from moisture). 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.
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. * In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
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.
Pureza y Documentación
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Ficha de datos (276 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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Instrucciones de manejo (2659 KB)
Referencias
[1]. Ward WH, et al. Ponalrestat: a potent and specific inhibitor of aldose reductase. Biochem Pharmacol. 1990 Jan 15;39(2):337-46. [Content Brief]
[2]. Bresson E, et al. The human aldose reductase AKR1B1 qualifies as the primary prostaglandin F synthase in the endometrium. J Clin Endocrinol Metab. 2011 Jan;96(1):210-9. [Content Brief]
[3]. Calcutt NA, et al. Prevention of sensory disorders in diabetic Sprague-Dawley rats by aldose reductase inhibition or treatment with ciliary neurotrophic factor. Diabetologia. 2004 Apr;47(4):718-24. [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 (sealed storage, away from moisture). 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 | 2.5563 mL | 12.7815 mL | 25.5630 mL | 63.9076 mL |
| 5 mM | 0.5113 mL | 2.5563 mL | 5.1126 mL | 12.7815 mL | |
| 10 mM | 0.2556 mL | 1.2782 mL | 2.5563 mL | 6.3908 mL | |
| 15 mM | 0.1704 mL | 0.8521 mL | 1.7042 mL | 4.2605 mL | |
| 20 mM | 0.1278 mL | 0.6391 mL | 1.2782 mL | 3.1954 mL | |
| 25 mM | 0.1023 mL | 0.5113 mL | 1.0225 mL | 2.5563 mL | |
| 30 mM | 0.0852 mL | 0.4261 mL | 0.8521 mL | 2.1303 mL | |
| 40 mM | 0.0639 mL | 0.3195 mL | 0.6391 mL | 1.5977 mL | |
| 50 mM | 0.0511 mL | 0.2556 mL | 0.5113 mL | 1.2782 mL | |
| 60 mM | 0.0426 mL | 0.2130 mL | 0.4261 mL | 1.0651 mL | |
| 80 mM | 0.0320 mL | 0.1598 mL | 0.3195 mL | 0.7988 mL | |
| 100 mM | 0.0256 mL | 0.1278 mL | 0.2556 mL | 0.6391 mL |
Ponalrestat Related Classifications
HY-106697 Related Classifications
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