A potent aldose reductase inhibitor (IC50s = 1.9 and 41 nM for the human placenta and rat lens enzymes

Zopolrestat – 1 mg

Brand:
Cayman
CAS:
110703-94-1
Storage:
-20
UN-No:
De Minimis - 2811 / 6.1

Zopolrestat is a potent inhibitor of aldose reductase (IC50s = 1.9 and 41 nM for the human placenta and rat lens enzymes, respectively).{48645} It inhibits sorbitol accumulation in human and rat erythrocytes (IC50s = 370 and 220 nM, respectively). Zopolrestat (50 μM) inhibits ethanol-induced aldose reductase activity and lipid accumulation in HepG2 cells.{48646} In vivo, zopolrestat (50 mg/kg) reduces sciatic nerve, retina, and lens accumulation of sorbitol in a rat model of diabetes induced by streptozotocin (STZ; Item No. 13104).{48645} It also reduces protein excretion and maintains lens transparency and myo-inositol content, markers of cataract development, in rats with STZ-induced diabetes when administered at a dose of 100 mg/kg.{48647} Zopolrestat also inhibits glyoxalase I (GLOI; Ki = 18 μM).{48648}  

 

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SKU: 29185 - 1 mg Category:

Description

A potent aldose reductase inhibitor (IC50s = 1.9 and 41 nM for the human placenta and rat lens enzymes, respectively); inhibits sorbitol accumulation in human and rat erythrocytes (IC50s = 370 and 220 nM, respectively); inhibits ethanol-induced aldose reductase activity and lipid accumulation in HepG2 cells at 50 μM; reduces sciatic nerve, retina, and lens accumulation of sorbitol in a rat model of STZ-induced diabetes at 50 mg/kg; reduces protein excretion and maintains lens transparency and myo-inositol content in rats with STZ-induced diabetes at 100 mg/kg; inhibits GLOI (Ki = 18 μM)

Formal name: 3,4-dihydro-4-oxo-3-[[5-(trifluoromethyl)-2-benzothiazolyl]methyl]-1-phthalazineacetic acid

Synonyms: 

Molecular weight: 419.4

CAS: 110703-94-1

Purity: ≥98%

Formulation: A crystalline solid

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