Epalrestat
Epalrestat structure
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Common Name | Epalrestat | ||
|---|---|---|---|---|
| CAS Number | 82159-09-9 | Molecular Weight | 319.399 | |
| Density | 1.4±0.1 g/cm3 | Boiling Point | 516.8±60.0 °C at 760 mmHg | |
| Molecular Formula | C15H13NO3S2 | Melting Point | 210-217ºC | |
| MSDS | Chinese USA | Flash Point | 266.4±32.9 °C | |
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Inhibitor selectivity between aldo–keto reductase superfamily members AKR1B10 and AKR1B1: Role of Trp112 (Trp111)
FEBS Lett. 587(22) , 3681-6, (2013) • Crystal structures of AKR1B10 holoenzyme. • Trp112 side-chain flipping in AKR1B10 explains non-selectivity of AKR1B1 inhibitors. • Native Trp112 side-chain orientation is critical for selective AKR1B10 inhibitors. |
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Docking and molecular dynamics studies toward the binding of new natural phenolic marine inhibitors and aldose reductase
J. Mol. Graph. Model. 28(2) , 162-9, (2009) Phenolic marine natural product is a kind of new potential aldose reductase inhibitors (ARIs). In order to investigate the binding mode and inhibition mechanism, molecular docking and dynamics studies were performed to explore the interactions of six phenolic... |
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6,7-Dihydroxy-4-phenylcoumarin as inhibitor of aldose reductase 2.
Bioorg. Med. Chem. Lett. 20 , 5630-3, (2010) We report the structure-activity relationship of a series of coumarins as aldose reductase 2 (ALR2) inhibitors and their suppressive effect on the accumulation of galactitol in the rat lens. We evaluated their ALR2 selectivity profile against sorbitol dehydro... |
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Inhibitory activities of prenylated flavonoids from Sophora flavescens against aldose reductase and generation of advanced glycation endproducts.
J. Pharm. Pharmacol. 60(9) , 1227-36, (2008) Important targets for the prevention and treatment of diabetic complications include aldose reductase (AR) inhibitors (ARIs) and inhibitors of advanced glycation endproduct (AGE) formation. Here we evaluate the inhibitory activities of prenylated flavonoids i... |
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Epalrestat. A review of its pharmacology, and therapeutic potential in late-onset complications of diabetes mellitus.
Drugs Aging 3(6) , 532-55, (1993) Epalrestat is a carboxylic acid derivative which inhibits aldose reductase, an enzyme of the sorbitol (polyol) pathway. Under hyperglycaemic conditions epalrestat reduces intracellular sorbitol accumulation, which has been implicated in the pathogenesis of la... |
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Molecular cloning and characterization of Schistosoma japonicum aldose reductase.
Parasitol. Res. 112(2) , 549-58, (2013) Antioxidant defense is an essential mechanism for schistosomes to cope with damage from host immune-generated reactive oxygen species. The evaluation of the effects of aldose reductase, an important enzyme that may be involved in this system, has long been ne... |
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Rhodanineacetic acid derivatives as potential drugs: preparation, hydrophobic properties and antifungal activity of (5-arylalkylidene-4-oxo-2-thioxo-1,3-thiazolidin-3-yl)acetic acids.
Molecules 14(10) , 4197-212, (2009) Some [(5Z)-(5-arylalkylidene-4-oxo-2-thioxo-1,3-thiazolidin-3-yl)]acetic acids were prepared as potential antifungal compounds. The general synthetic approach to all synthesized compounds is presented. Lipophilicity of all the discussed rhodanine-3-acetic aci... |
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LC-MS/MS method for the quantification of aldose reductase inhibitor-epalrestat and application to pharmacokinetic study.
J. Pharm. Biomed. Anal. 74 , 227-34, (2013) A simple and rapid LC-MS/MS method was developed and validated for the quantification of epalrestat, an aldose reductase inhibitor for the treatment of diabetic neuropathy. Following protein precipitation epalrestat and IS were eluted with 10mM ammonium aceta... |
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Effects of epalrestat, an aldose reductase inhibitor, on diabetic peripheral neuropathy in patients with type 2 diabetes, in relation to suppression ofNɛ-carboxymethyl lysine
J. Diabetes Complications 24(6) , 424-32, (2010) Objective We investigated the efficacy of epalrestat, an aldose reductase inhibitor, for diabetic peripheral neuropathy in Japanese patients with type 2 diabetes. |
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Anti-ischaemic activity of an antioxidant aldose reductase inhibitor on diabetic and non-diabetic rat hearts.
J. Pharm. Pharmacol. 62(1) , 107-13, (2010) Many observations report the cardioprotective effects of inhibitors of aldose reductase in different models of ischaemia-reperfusion injury in diabetic myocardium. In this paper, the inhibitory effects of the new pyrido[1,2-a]-pyrimidin-4-one derivative PPO, ... |