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Zopolrestat

Catalog No. T35317 CAS 110703-94-1

Synonyms: CP-73850, Zopolrestatum, CP73850, CP 73850

Zopolrestat is a potent inhibitor of aldose Reductase (IC50 = 3.1 nM).

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Zopolrestat, CAS 110703-94-1

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Purity: 98%

Biological Description

Chemical Properties

Storage & Solubility Information

Description	Zopolrestat is a potent inhibitor of aldose reductase (IC50 = 3.1 nM).
Targets&IC50	Aldose reductase:3.1 nM
In vitro	Zopolrestat is a potent inhibitor of the enzymatic reduction of glyceraldehyde and glucose[1].
In vivo	After the administration of Zopolrestat (2.5 mg/kg-50 mg/kg; p.o), the 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[1].

Synonyms	CP-73850, Zopolrestatum, CP73850, CP 73850
Molecular Weight	419.38
Formula	C19H12F3N3O3S
CAS No.	110703-94-1

Storage

Powder: -20°C for 3 years

In solvent: -80°C for 2 years

Solubility Information

DMSO: 11 mg/mL (26.23 mM), Need ultrasonic

( < 1 mg/ml refers to the product slightly soluble or insoluble )

References and Literature

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. 2. Zhai J, et al. Zopolrestat as a human glyoxalase I inhibitor and its structural basis. ChemMedChem. 2013 Sep;8(9):1462-4. 3. Badawy D, et al. Aldose reductase inhibitors zopolrestat and ferulic acid alleviate hypertension associated with diabetes: effect on vascular reactivity. Can J Physiol Pharmacol. 2013 Feb;91(2):101-7. 4. Ramasamy R, et al. Attenuation of ischemia induced increases in sodium and calcium by the aldose reductase inhibitor zopolrestat. Cardiovasc Res. 1999 Apr;42(1):130-9.

Dose Conversion

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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO (Master liquid concentration mg/mL)，Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.

Method for preparing in vivo formulation：Take μL DMSO master liquid, next add μL PEG300， mix and clarify, next add μL Tween 80，mix and clarify, next add μL ddH₂O, mix and clarify.

Note:

Be sure to add the solvent(s) in order. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.

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Tech Support

Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc.

Keywords

Zopolrestat 110703-94-1 Endocrinology/Hormones Metabolism Reductase CP-73850 diabetic potent glyceraldehyde Zopolrestatum glucose aldose CP73850 rats inhibit Aldose Reductase Inhibitor CP 73850 oral inhibitor

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