110703-94-1

110703-94-1 structure

Name: CP 73850
Chemical Name: Zopolrestat
CAS Number: 110703-94-1
Molecular Formula: C₁₉H₁₂F₃N₃O₃S
Molecular Weight: 419.37700
Catalog: Signaling Pathways Metabolic Enzyme/Protease Aldose Reductase
Create Date: 2018-09-25 13:26:13
Modify Date: 2024-01-06 16:12:04
Zopolrestat (CP73850) is a potent, orally active aldose reductase (AR) inhibitor with an IC50 of 3.1 nM. Zopolrestat is used for the research of diabetic complications[1].

Name	Zopolrestat
Synonyms	2-[4-oxo-3-[[5-(trifluoromethyl)-1,3-benzothiazol-2-yl]methyl]phthalazin-1-yl]acetic acid

Description	Zopolrestat (CP73850) is a potent, orally active aldose reductase (AR) inhibitor with an IC50 of 3.1 nM. Zopolrestat is used for the research of diabetic complications[1].
Related Catalog	Signaling Pathways >> Metabolic Enzyme/Protease >> Aldose Reductase Research Areas >> Metabolic Disease
In Vitro	Zopolrestat is a potent inhibitor of the reduction of both glyceraldehyde and glucose by the human and rat enzymes[1].
In Vivo	Zopolrestat (2.5 mg/kg-50 mg/kg; p.o.; once-a-day for 5 days) and left untreated for 7 days) prevents accumulation of sorbitol in the kidney cortex of diabetic rats and normalize elevated renal blood flow in galactosemic rats[1]. Animal Model: Male Sprague-Dawley rats (made diabetic by iv injection of streptozotocin)[1]. Dosage: 2.5 mg/kg-50 mg/kg Administration: P.o.; once-a-day for 5 days Result: Its ED50s in reversing already elevated sorbitol accumulation in rat sciatic nerve, retina, and lens in a chronic test were 1.9, 17.6, and 18.4 mg/kg, respectively.
References	[1]. Mylari BL, et al. Novel, potent aldose reductase inhibitors: 3,4-dihydro-4-oxo-3-[[5-(trifluoromethyl)-2-benzothiazolyl] methyl]-1-phthalazineacetic acid (zopolrestat) and congeners. J Med Chem. 1991;34(1):108-122.