Zopolrestat
- Product Name
- Zopolrestat
- CAS No.
- 110703-94-1
- Chemical Name
- Zopolrestat
- Synonyms
- Xedia;Alond;CP-73850;Zopalrestat;Zopolrestatum;Zopolrestat, CP-73850;Zopolrestat >=98% (HPLC);Zopolrestat, 10 mM in DMSO;BCSVCWVQNOXFGL-UHFFFAOYSA-N;3-[(5-Trifluoromethyl-2-benzothiazolyl)methyl]-3,4-dihydro-4-oxophthalazine-1-acetic acid
- CBNumber
- CB41180112
- Molecular Formula
- C19H12F3N3O3S
- Formula Weight
- 419.38
- MOL File
- 110703-94-1.mol
Zopolrestat Property
- Melting point:
- 197-198℃
- Density
- 1.58
- storage temp.
- 2-8°C
- solubility
- DMSO: ≥20mg/mL
- pka
- pKa (dioxane/water): 5.46 (1:1); 6.38 (2:1)
- form
- powder
- color
- off-white to light brown
N-Bromosuccinimide Price
- Product number
- Z4527
- Product name
- Zopolrestat
- Purity
- ≥98% (HPLC)
- Packaging
- 10mg
- Price
- $125
- Updated
- 2025/07/31
- Product number
- Z4527
- Product name
- Zopolrestat
- Purity
- ≥98% (HPLC)
- Packaging
- 50mg
- Price
- $488
- Updated
- 2025/07/31
- Product number
- 29185
- Product name
- Zopolrestat
- Packaging
- 1mg
- Price
- $32
- Updated
- 2024/03/01
- Product number
- 29185
- Product name
- Zopolrestat
- Packaging
- 5mg
- Price
- $116
- Updated
- 2024/03/01
- Product number
- 29185
- Product name
- Zopolrestat
- Packaging
- 10mg
- Price
- $214
- Updated
- 2024/03/01
Zopolrestat Chemical Properties,Usage,Production
Originator
Alond,Pfizer
Uses
Antidiabetic; inhibitor (aldose reductase).
Manufacturing Process
A mixture of 2-methyl-5-trifluoromethylbenzothiazole (1 mole-equivalent), N- bromosuccinimide (1 mole-equivalent), carbon tetrachloride (700 ml) and a catalytic amount of benzoyl peroxide (0.2 g) was refluxed under irradiation by an UV lamp for 14 hours. The reaction mixture was cooled to room temperature, filtered to remove the precipitated succinimide and the filtrate was evaporated to dryness. The resulting solid was chromatographed over silica gel to obtain the 2-bromomethyl-5-trifluoromethyl-benzothiazole. To a mixture of ethyl 4-oxo-3H-phthalazin-1-ylacetate (1 mole-equivalent) and sodium hydride (50% w/w dispersion in mineral oil) in dimethylformamide (150 ml) was added 2-bromomethyl-5-trifluoromethylbenzothiazole (1 mole- equivalent) and the resulting mixture stirred at room temperature for 1 hour. This reaction mixture was poured over ice-water (500 ml); sufficient 10% HCl was added to adjust the pH to about 4.0 and the precipitated crude solid was collected. This was chromatographed over silica gel to obtain the ethyl[4-oxo- 3-(5-trifluoromethylbenzothiazol-2-yl)-3,4-dihydro-phthalazin-1-yl]acetate; MP: 134°-136°C. A solution of methyl or ethyl [4-oxo-3-(5-trifluoromethylbenzothiazol-2-yl)- 3,4-dihydrophthalazin-1-yl]acetate (1 mole-equivalent) in methanol (50 ml)
Therapeutic Function
Aldose reductase inhibitor
Biological Activity
Zopolrest at is an inhibitor of Aldose Reductase. AR family members AKR1B1 and AKR1B10 have additionally been shown to play roles in inflammation and cancer.
Zopolrestat Preparation Products And Raw materials
Raw materials
Preparation Products
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