An aldose reductase inhibitor (IC50s = 0.01 and 0.26 µM for rat lens and human placenta aldose reductase

Epalrestat – 25 mg

Brand:
Cayman
CAS:
82159-09-9
Storage:
-20
UN-No:
Non-Hazardous - /

Epalrestat is an inhibitor of aldose reductase (IC50s = 0.01 and 0.26 µM for rat lens and human placenta aldose reductase, respectively).{53254} It inhibits glucose-induced sorbitol accumulation in isolated rat lens, rat sciatic nerve, and human erythrocytes (IC50s = 1.5, 5, and 1.5 µM, respectively). It decreases high glucose-induced proliferation of vascular smooth muscle cells when used at a concentration of 10 nM and prevents high glucose-induced intracellular NADH/NAD+ increases and membrane-bound PKC activation at 100 nM.{24663,24664} Epalrestat (20 and 40 mg/kg) improves motor nerve conduction velocity and decreases sorbitol content in the sciatic nerve and erythrocytes in a rat model of streptozotocin-induced diabetic neuropathy.{53255} It also prevents capillary strand formation in a rat model of diabetes-induced retinal microangiopathy when administered at a dose of 50 mg/kg.{53256}  

 

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Description

An aldose reductase inhibitor (IC50s = 0.01 and 0.26 µM for rat lens and human placenta aldose reductase, respectively); inhibits glucose-induced sorbitol accumulation in isolated rat lens, rat sciatic nerve, and human erythrocytes (IC50s = 1.5, 5, and 1.5 µM, respectively); decreases high glucose-induced proliferation of vascular smooth muscle cells at 10 nM and prevents high glucose-induced intracellular NADH/NAD+ increases and membrane-bound PKC activation at 100 nM; improves motor nerve conduction velocity and decreases sorbitol content in the sciatic nerve and erythrocytes in a rat model of streptozotocin-induced diabetic neuropathy at 20 and 40 mg/kg; prevents capillary strand formation in a rat model of diabetes-induced retinal microangiopathy at 50 mg/kg

Formal name: 5Z-[(2E)-2-methyl-3-phenyl-2-propen-1-ylidene]-4-oxo-2-thioxo-3-thiazolidineacetic acid

Synonyms:  ONO-2235

Molecular weight: 319.4

CAS: 82159-09-9

Purity: ≥98%

Formulation: A crystalline solid

Product Type|Biochemicals|Small Molecule Inhibitors||Research Area|Cardiovascular System|Blood|Erythrocytes & Hemoglobin||Research Area|Cardiovascular System|Vasculature|Angiogenesis||Research Area|Cardiovascular System|Vasculature|Smooth Muscle Cells||Research Area|Endocrinology & Metabolism|Carbohydrate Metabolism||Research Area|Neuroscience

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