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Literature summary extracted from

  • Qin, X.; Hao, X.; Han, H.; Zhu, S.; Yang, Y.; Wu, B.; Hussain, S.; Parveen, S.; Jing, C.; Ma, B.; Zhu, C.
    Design and synthesis of potent and multifunctional aldose reductase inhibitors based on quinoxalinones (2015), J. Med. Chem., 58, 1254-1267.
    View publication on PubMed

Inhibitors

EC Number Inhibitors Comment Organism Structure
1.1.1.2 (3-benzyl-2-oxoquinoxalin-1(2H)-yl)acetic acid 32.8% inhibition at 0.010 mM Rattus norvegicus
1.1.1.2 2-(3,7-bis(4-fluorophenyl)-2-oxoquinoxalin-1(2H)-yl)acetic acid 41.0% inhibition at 0.010 mM Rattus norvegicus
1.1.1.2 2-(3-(2,4-dihydroxyphenyl)-2-oxoquinoxalin-1(2H)-yl)acetic acid 36.6% inhibition at 0.010 mM Rattus norvegicus
1.1.1.2 2-(3-(3-indolyl)-2-oxoquinoxalin-1(2H)-yl)acetic acid 32.3% inhibition at 0.010 mM Rattus norvegicus
1.1.1.2 2-(3-(4-bromothiophenoxy)-2-oxoquinoxalin-1(2H)-yl)acetic acid 12.8% inhibition at 0.010 mM Rattus norvegicus
1.1.1.2 2-(3-(4-chlorothiophenoxy)-2-oxoquinoxalin-1(2H)-yl)acetic acid 42.4% inhibition at 0.010 mM Rattus norvegicus
1.1.1.2 2-(3-(4-fluorophenyl)-2-oxoquinoxalin-1(2H)-yl)acetic acid 31.8% inhibition at 0.010 mM Rattus norvegicus
1.1.1.2 2-(3-(4-hydroxyphenyl)-2-oxoquinoxalin-1(2H)-yl)acetic acid 34.6% inhibition at 0.010 mM Rattus norvegicus
1.1.1.2 2-(3-phenoxy-2-oxoquinoxalin-1(2H)-yl)acetic acid 6.6% inhibition at 0.010 mM Rattus norvegicus
1.1.1.2 2-(3-phenyl-2-oxoquinoxalin-1(2H)-yl)acetic acid 25.4% inhibition at 0.010 mM Rattus norvegicus
1.1.1.2 2-(3-thiophenoxy-2-oxoquinoxalin-1(2H)-yl)acetic acid 32.2% inhibition at 0.010 mM Rattus norvegicus
1.1.1.2 2-(6-bromo-3-(2,4-dihydroxyphenyl)-2-oxoquinoxalin-1(2H)-yl)-acetic acid 38.1% inhibition at 0.010 mM Rattus norvegicus
1.1.1.2 2-(6-bromo-3-(4-bromothiophenoxy)-2-oxoquinoxalin-1(2H)-yl)-acetic acid 8.7% inhibition at 0.010 mM Rattus norvegicus
1.1.1.2 2-(6-chloro-3-(2,4-dihydroxyphenyl)-2-oxoquinoxalin-1(2H)-yl)-acetic acid 46.5% inhibition at 0.010 mM Rattus norvegicus
1.1.1.2 2-(6-fluoro-3-(2,4-dihydroxyphenyl)-2-oxoquinoxalin-1(2H)-yl)-acetic acid 42.5% inhibition at 0.010 mM Rattus norvegicus
1.1.1.2 2-(7-(4-fluorobenzyl)-3-(2,4-dihydroxyphenyl)-2-oxoquinoxalin-1(2H)-yl)acetic acid 11.6% inhibition at 0.010 mM Rattus norvegicus
1.1.1.2 2-(7-bromo-3-(2,4-dihydroxyphenyl)-2-oxoquinoxalin-1(2H)-yl)-acetic acid 35.9% inhibition at 0.010 mM Rattus norvegicus
1.1.1.2 2-(7-bromo-3-(3-indolyl)-2-oxoquinoxalin-1(2H)-yl)acetic acid 17.5% inhibition at 0.010 mM Rattus norvegicus
1.1.1.2 2-(7-bromo-3-(4-bromothiophenoxy)-2-oxoquinoxalin-1(2H)-yl)-acetic acid 24.0% inhibition at 0.010 mM Rattus norvegicus
1.1.1.2 2-(7-bromo-3-(4-chlorothiophenoxy)-2-oxoquinoxalin-1(2H)-yl)-acetic acid 10.2% inhibition at 0.010 mM Rattus norvegicus
1.1.1.2 2-(7-chloro-3-(2,4-dihydroxyphenyl)-2-oxoquinoxalin-1(2H)-yl)-acetic acid 44.5% inhibition at 0.010 mM Rattus norvegicus
1.1.1.2 2-(7-chloro-3-(2-benzothiophene)-2-oxoquinoxalin-1(2H)-yl)-acetic acid 53.3% inhibition at 0.010 mM Rattus norvegicus
1.1.1.2 2-(7-chloro-3-(4-bromothiophenoxy)-2-oxoquinoxalin-1(2H)-yl)-acetic acid 14.1% inhibition at 0.010 mM Rattus norvegicus
1.1.1.2 2-(7-chloro-3-(4-chlorothiophenoxy)-2-oxoquinoxalin-1(2H)-yl)-acetic acid 17.3% inhibition at 0.010 mM Rattus norvegicus
1.1.1.2 2-(7-chloro-3-(4-fluorophenyl)-2-oxoquinoxalin-1(2H)-yl)acetic acid 23.6% inhibition at 0.010 mM Rattus norvegicus
1.1.1.2 2-(7-fluoro-3-(2,4-dihydroxyphenyl)-2-oxoquinoxalin-1(2H)-yl)-acetic acid 46.2% inhibition at 0.010 mM Rattus norvegicus
1.1.1.2 2-(7-fluoro-3-(4-bromothiophenoxy)-2-oxoquinoxalin-1(2H)-yl)-acetic acid 45.5% inhibition at 0.010 mM Rattus norvegicus
1.1.1.2 2-(7-fluoro-3-(4-chlorothiophenoxy)-2-oxoquinoxalin-1(2H)-yl)-acetic acid 29.5% inhibition at 0.010 mM Rattus norvegicus
1.1.1.2 2-(7-fluoro-3-(4-fluorophenyl)-2-oxoquinoxalin-1(2H)-yl)acetic acid 35.8% inhibition at 0.010 mM Rattus norvegicus
1.1.1.2 epalrestat 73.6% inhibition at 0.010 mM Rattus norvegicus
1.1.1.2 additional information design and synthesis of inhibitors based on quinoxalinones, overview. Phenolic structure is installed in the compounds for the combination of antioxidant activity and strengthening the ability to fight against diabetic complications, radical scavenging activity using the model reaction with the stable free radicals of 2,2-diphenyl-1-picrylhydrazyl Rattus norvegicus
1.1.1.2 [2-oxo-3-(2-phenylethyl)quinoxalin-1(2H)-yl]acetic acid 22.0% inhibition at 0.010 mM Rattus norvegicus
1.1.1.2 [2-oxo-3-[(Z)-2-phenylethenyl]quinoxalin-1(2H)-yl]acetic acid 32.0% inhibition at 0.010 mM Rattus norvegicus
1.1.1.2 [3-[(E)-2-(4-hydroxy-3-methoxyphenyl)ethenyl]-2-oxoquinoxalin-1(2H)-yl]acetic acid 32.6% inhibition at 0.010 mM Rattus norvegicus
1.1.1.2 [3-[(E)-2-(4-hydroxyphenyl)ethenyl]-2-oxoquinoxalin-1(2H)-yl]acetic acid 42.4% inhibition at 0.010 mM Rattus norvegicus
1.1.1.2 [3-[(E)-2-(4-methoxyphenyl)ethenyl]-2-oxoquinoxalin-1(2H)-yl]acetic acid 21.8% inhibition at 0.010 mM Rattus norvegicus
1.1.1.2 [3-[2-(4-hydroxyphenyl)ethyl]-2-oxoquinoxalin-1(2H)-yl]acetic acid 12.2% inhibition at 0.010 mM Rattus norvegicus
1.1.1.2 [7-fluoro-3-[(E)-2-(4-hydroxyphenyl)ethenyl]-2-oxoquinoxalin-1(2H)-yl]acetic acid 36.2% inhibition at 0.010 mM Rattus norvegicus
1.1.1.2 [7-fluoro-3-[2-(4-hydroxyphenyl)ethyl]-2-oxoquinoxalin-1(2H)-yl]acetic acid 23.0% inhibition at 0.010 mM Rattus norvegicus
1.1.1.21 (3-benzyl-2-oxoquinoxalin-1(2H)-yl)acetic acid
-
 Rattus norvegicus
1.1.1.21 1,2-benzothiazin-1,1-dioxide
-
 Rattus norvegicus
1.1.1.21 2-(3,7-bis(4-fluorophenyl)-2-oxoquinoxalin-1(2H)-yl)acetic acid
-
 Rattus norvegicus
1.1.1.21 2-(3-(2,4-dihydroxyphenyl)-2-oxoquinoxalin-1(2H)-yl)acetic acid
-
 Rattus norvegicus
1.1.1.21 2-(3-(3-indolyl)-2-oxoquinoxalin-1(2H)-yl)acetic acid
-
 Rattus norvegicus
1.1.1.21 2-(3-(4-bromothiophenoxy)-2-oxoquinoxalin-1(2H)-yl)acetic acid
-
 Rattus norvegicus
1.1.1.21 2-(3-(4-chlorothiophenoxy)-2-oxoquinoxalin-1(2H)-yl)acetic acid
-
 Rattus norvegicus
1.1.1.21 2-(3-(4-fluorophenyl)-2-oxoquinoxalin-1(2H)-yl)acetic acid
-
 Rattus norvegicus
1.1.1.21 2-(3-(4-hydroxyphenyl)-2-oxoquinoxalin-1(2H)-yl)acetic acid
-
 Rattus norvegicus
1.1.1.21 2-(3-phenoxy-2-oxoquinoxalin-1(2H)-yl)acetic acid
-
 Rattus norvegicus
1.1.1.21 2-(3-phenyl-2-oxoquinoxalin-1(2H)-yl)acetic acid
-
 Rattus norvegicus
1.1.1.21 2-(3-thiophenoxy-2-oxoquinoxalin-1(2H)-yl)acetic acid
-
 Rattus norvegicus
1.1.1.21 2-(6-bromo-3-(2,4-dihydroxyphenyl)-2-oxoquinoxalin-1(2H)-yl)-acetic acid
-
 Rattus norvegicus
1.1.1.21 2-(6-bromo-3-(4-bromothiophenoxy)-2-oxoquinoxalin-1(2H)-yl)-acetic acid
-
 Rattus norvegicus
1.1.1.21 2-(6-chloro-3-(2,4-dihydroxyphenyl)-2-oxoquinoxalin-1(2H)-yl)-acetic acid
-
 Rattus norvegicus
1.1.1.21 2-(6-fluoro-3-(2,4-dihydroxyphenyl)-2-oxoquinoxalin-1(2H)-yl)-acetic acid
-
 Rattus norvegicus
1.1.1.21 2-(7-(4-fluorobenzyl)-3-(2,4-dihydroxyphenyl)-2-oxoquinoxalin-1(2H)-yl)acetic acid
-
 Rattus norvegicus
1.1.1.21 2-(7-bromo-3-(2,4-dihydroxyphenyl)-2-oxoquinoxalin-1(2H)-yl)-acetic acid
-
 Rattus norvegicus
1.1.1.21 2-(7-bromo-3-(3-indolyl)-2-oxoquinoxalin-1(2H)-yl)acetic acid
-
 Rattus norvegicus
1.1.1.21 2-(7-bromo-3-(4-bromothiophenoxy)-2-oxoquinoxalin-1(2H)-yl)-acetic acid
-
 Rattus norvegicus
1.1.1.21 2-(7-bromo-3-(4-chlorothiophenoxy)-2-oxoquinoxalin-1(2H)-yl)-acetic acid
-
 Rattus norvegicus
1.1.1.21 2-(7-chloro-3-(2,4-dihydroxyphenyl)-2-oxoquinoxalin-1(2H)-yl)-acetic acid
-
 Rattus norvegicus
1.1.1.21 2-(7-chloro-3-(2-benzothiophene)-2-oxoquinoxalin-1(2H)-yl)-acetic acid
-
 Rattus norvegicus
1.1.1.21 2-(7-chloro-3-(4-bromothiophenoxy)-2-oxoquinoxalin-1(2H)-yl)-acetic acid
-
 Rattus norvegicus
1.1.1.21 2-(7-chloro-3-(4-chlorothiophenoxy)-2-oxoquinoxalin-1(2H)-yl)-acetic acid
-
 Rattus norvegicus
1.1.1.21 2-(7-chloro-3-(4-fluorophenyl)-2-oxoquinoxalin-1(2H)-yl)acetic acid
-
 Rattus norvegicus
1.1.1.21 2-(7-fluoro-3-(2,4-dihydroxyphenyl)-2-oxoquinoxalin-1(2H)-yl)-acetic acid
-
 Rattus norvegicus
1.1.1.21 2-(7-fluoro-3-(4-bromothiophenoxy)-2-oxoquinoxalin-1(2H)-yl)-acetic acid
-
 Rattus norvegicus
1.1.1.21 2-(7-fluoro-3-(4-chlorothiophenoxy)-2-oxoquinoxalin-1(2H)-yl)-acetic acid
-
 Rattus norvegicus
1.1.1.21 2-(7-fluoro-3-(4-fluorophenyl)-2-oxoquinoxalin-1(2H)-yl)acetic acid
-
 Rattus norvegicus
1.1.1.21 6-(5-chloro,3-methylbenzofuran-2-sulfonyl)2H-pyridazin-3-one
-
 Rattus norvegicus
1.1.1.21 epalrestat
-
 Rattus norvegicus
1.1.1.21 fidarestat
-
 Rattus norvegicus
1.1.1.21 lidorestat
-
 Rattus norvegicus
1.1.1.21 additional information design and synthesis of potent and multifunctional aldose reductase inhibitors based on quinoxalinones, overview. Phenolic structure is installed in the compounds for the combination of antioxidant activity and strengthening the ability to fight against diabetic complications, radical scavenging activity using the model reaction with the stable free radicals of 2,2-diphenyl-1-picrylhydrazyl. Molecular docking study using the lidorestat-bound conformation of ALR2, PDB ID 1Z3N Rattus norvegicus
1.1.1.21 ponalrestat
-
 Rattus norvegicus
1.1.1.21 sorbinil
-
 Rattus norvegicus
1.1.1.21 zenorestat
-
 Rattus norvegicus
1.1.1.21 [2-oxo-3-(2-phenylethyl)quinoxalin-1(2H)-yl]acetic acid
-
 Rattus norvegicus
1.1.1.21 [2-oxo-3-[(Z)-2-phenylethenyl]quinoxalin-1(2H)-yl]acetic acid
-
 Rattus norvegicus
1.1.1.21 [3-[(E)-2-(4-hydroxy-3-methoxyphenyl)ethenyl]-2-oxoquinoxalin-1(2H)-yl]acetic acid
-
 Rattus norvegicus
1.1.1.21 [3-[(E)-2-(4-hydroxyphenyl)ethenyl]-2-oxoquinoxalin-1(2H)-yl]acetic acid
-
 Rattus norvegicus
1.1.1.21 [3-[(E)-2-(4-methoxyphenyl)ethenyl]-2-oxoquinoxalin-1(2H)-yl]acetic acid
-
 Rattus norvegicus
1.1.1.21 [3-[2-(4-hydroxyphenyl)ethyl]-2-oxoquinoxalin-1(2H)-yl]acetic acid
-
 Rattus norvegicus
1.1.1.21 [7-fluoro-3-[(E)-2-(4-hydroxyphenyl)ethenyl]-2-oxoquinoxalin-1(2H)-yl]acetic acid
-
 Rattus norvegicus
1.1.1.21 [7-fluoro-3-[2-(4-hydroxyphenyl)ethyl]-2-oxoquinoxalin-1(2H)-yl]acetic acid
-
 Rattus norvegicus

Natural Substrates/ Products (Substrates)

EC Number Natural Substrates Organism Comment (Nat. Sub.) Natural Products Comment (Nat. Pro.) Rev. Reac.
1.1.1.2 D-glucose + NADPH + H+ Rattus norvegicus
-
 sorbitol + NADP+
-
 ?
1.1.1.2 D-glucose + NADPH + H+ Rattus norvegicus Wistar
-
 sorbitol + NADP+
-
 ?
1.1.1.21 D-glucose + NADPH + H+ Rattus norvegicus
-
 sorbitol + NADP+
-
 ?
1.1.1.21 D-glucose + NADPH + H+ Rattus norvegicus Wistar
-
 sorbitol + NADP+
-
 ?

Organism

EC Number Organism UniProt Comment Textmining
1.1.1.2 Rattus norvegicus P51635
-
-
1.1.1.2 Rattus norvegicus Wistar P51635
-
-
1.1.1.21 Rattus norvegicus P07943
-
-
1.1.1.21 Rattus norvegicus Wistar P07943
-
-

Substrates and Products (Substrate)

EC Number Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
1.1.1.2 D-glucose + NADPH + H+
-
 Rattus norvegicus sorbitol + NADP+
-
 ?
1.1.1.2 D-glucose + NADPH + H+
-
 Rattus norvegicus Wistar sorbitol + NADP+
-
 ?
1.1.1.2 DL-glyceraldehyde + NADPH + H+
-
 Rattus norvegicus ? + NADP+
-
 ?
1.1.1.2 DL-glyceraldehyde + NADPH + H+
-
 Rattus norvegicus Wistar ? + NADP+
-
 ?
1.1.1.21 D-glucose + NADPH + H+
-
 Rattus norvegicus sorbitol + NADP+
-
 ?
1.1.1.21 D-glucose + NADPH + H+
-
 Rattus norvegicus Wistar sorbitol + NADP+
-
 ?
1.1.1.21 DL-glyceraldehyde + NADPH + H+
-
 Rattus norvegicus glycerol + NADP+
-
 ?
1.1.1.21 DL-glyceraldehyde + NADPH + H+
-
 Rattus norvegicus Wistar glycerol + NADP+
-
 ?

Synonyms

EC Number Synonyms Comment Organism
1.1.1.2 AKR1A1
-
 Rattus norvegicus
1.1.1.2 aldose reductase
-
 Rattus norvegicus
1.1.1.2 ALR1
-
 Rattus norvegicus
1.1.1.21 AKR1B1
-
 Rattus norvegicus
1.1.1.21 aldose reductase
-
 Rattus norvegicus
1.1.1.21 ALR2
-
 Rattus norvegicus

Temperature Optimum [°C]

EC Number Temperature Optimum [°C] Temperature Optimum Maximum [°C] Comment Organism
1.1.1.2 37
-
 assay at Rattus norvegicus
1.1.1.21 30
-
 assay at Rattus norvegicus

pH Optimum

EC Number pH Optimum Minimum pH Optimum Maximum Comment Organism
1.1.1.2 7.2
-
 assay at Rattus norvegicus
1.1.1.21 6.2
-
 assay at Rattus norvegicus

Cofactor

EC Number Cofactor Comment Organism Structure
1.1.1.2 NADPH
-
 Rattus norvegicus
1.1.1.21 NADPH
-
 Rattus norvegicus

IC50 Value

EC Number IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
1.1.1.21 0.000032
-
 pH 6.2, 30°C Rattus norvegicus 2-(7-fluoro-3-(2,4-dihydroxyphenyl)-2-oxoquinoxalin-1(2H)-yl)-acetic acid
1.1.1.21 0.000056
-
 pH 6.2, 30°C Rattus norvegicus 2-(7-fluoro-3-(4-chlorothiophenoxy)-2-oxoquinoxalin-1(2H)-yl)-acetic acid
1.1.1.21 0.00006
-
 pH 6.2, 30°C Rattus norvegicus 2-(6-fluoro-3-(2,4-dihydroxyphenyl)-2-oxoquinoxalin-1(2H)-yl)-acetic acid
1.1.1.21 0.000069
-
 pH 6.2, 30°C Rattus norvegicus 2-(7-chloro-3-(2,4-dihydroxyphenyl)-2-oxoquinoxalin-1(2H)-yl)-acetic acid
1.1.1.21 0.000084
-
 pH 6.2, 30°C Rattus norvegicus epalrestat
1.1.1.21 0.000091
-
 pH 6.2, 30°C Rattus norvegicus 2-(7-bromo-3-(2,4-dihydroxyphenyl)-2-oxoquinoxalin-1(2H)-yl)-acetic acid
1.1.1.21 0.000095
-
 pH 6.2, 30°C Rattus norvegicus 2-(6-chloro-3-(2,4-dihydroxyphenyl)-2-oxoquinoxalin-1(2H)-yl)-acetic acid
1.1.1.21 0.000139
-
 pH 6.2, 30°C Rattus norvegicus 2-(6-bromo-3-(2,4-dihydroxyphenyl)-2-oxoquinoxalin-1(2H)-yl)-acetic acid
1.1.1.21 0.00014
-
 pH 6.2, 30°C Rattus norvegicus [2-oxo-3-(2-phenylethyl)quinoxalin-1(2H)-yl]acetic acid
1.1.1.21 0.000153
-
 pH 6.2, 30°C Rattus norvegicus [7-fluoro-3-[(E)-2-(4-hydroxyphenyl)ethenyl]-2-oxoquinoxalin-1(2H)-yl]acetic acid
1.1.1.21 0.000158
-
 pH 6.2, 30°C Rattus norvegicus 2-(7-chloro-3-(4-chlorothiophenoxy)-2-oxoquinoxalin-1(2H)-yl)-acetic acid
1.1.1.21 0.00018
-
 pH 6.2, 30°C Rattus norvegicus [3-[(E)-2-(4-hydroxyphenyl)ethenyl]-2-oxoquinoxalin-1(2H)-yl]acetic acid
1.1.1.21 0.00019
-
 pH 6.2, 30°C Rattus norvegicus 2-(7-fluoro-3-(4-bromothiophenoxy)-2-oxoquinoxalin-1(2H)-yl)-acetic acid
1.1.1.21 0.000238
-
 pH 6.2, 30°C Rattus norvegicus 2-(7-chloro-3-(2-benzothiophene)-2-oxoquinoxalin-1(2H)-yl)-acetic acid
1.1.1.21 0.00027
-
 pH 6.2, 30°C Rattus norvegicus 2-(3-(4-chlorothiophenoxy)-2-oxoquinoxalin-1(2H)-yl)acetic acid
1.1.1.21 0.000296
-
 pH 6.2, 30°C Rattus norvegicus 2-(3-(4-bromothiophenoxy)-2-oxoquinoxalin-1(2H)-yl)acetic acid
1.1.1.21 0.000319
-
 pH 6.2, 30°C Rattus norvegicus 2-(6-bromo-3-(4-bromothiophenoxy)-2-oxoquinoxalin-1(2H)-yl)-acetic acid
1.1.1.21 0.000326
-
 pH 6.2, 30°C Rattus norvegicus 2-(7-chloro-3-(4-bromothiophenoxy)-2-oxoquinoxalin-1(2H)-yl)-acetic acid
1.1.1.21 0.000368
-
 pH 6.2, 30°C Rattus norvegicus 2-(7-bromo-3-(3-indolyl)-2-oxoquinoxalin-1(2H)-yl)acetic acid
1.1.1.21 0.000395
-
 pH 6.2, 30°C Rattus norvegicus 2-(7-bromo-3-(4-chlorothiophenoxy)-2-oxoquinoxalin-1(2H)-yl)-acetic acid
1.1.1.21 0.0004
-
 pH 6.2, 30°C Rattus norvegicus 2-(3-(2,4-dihydroxyphenyl)-2-oxoquinoxalin-1(2H)-yl)acetic acid
1.1.1.21 0.000419
-
 pH 6.2, 30°C Rattus norvegicus [3-[(E)-2-(4-hydroxy-3-methoxyphenyl)ethenyl]-2-oxoquinoxalin-1(2H)-yl]acetic acid
1.1.1.21 0.00042
-
 pH 6.2, 30°C Rattus norvegicus 2-(3-thiophenoxy-2-oxoquinoxalin-1(2H)-yl)acetic acid
1.1.1.21 0.000467
-
 pH 6.2, 30°C Rattus norvegicus 2-(7-bromo-3-(4-bromothiophenoxy)-2-oxoquinoxalin-1(2H)-yl)-acetic acid
1.1.1.21 0.000468
-
 pH 6.2, 30°C Rattus norvegicus 2-(3-phenoxy-2-oxoquinoxalin-1(2H)-yl)acetic acid
1.1.1.21 0.000639
-
 pH 6.2, 30°C Rattus norvegicus 2-(3-(3-indolyl)-2-oxoquinoxalin-1(2H)-yl)acetic acid
1.1.1.21 0.00065
-
 pH 6.2, 30°C Rattus norvegicus [7-fluoro-3-[2-(4-hydroxyphenyl)ethyl]-2-oxoquinoxalin-1(2H)-yl]acetic acid
1.1.1.21 0.0008
-
 pH 6.2, 30°C Rattus norvegicus [3-[2-(4-hydroxyphenyl)ethyl]-2-oxoquinoxalin-1(2H)-yl]acetic acid
1.1.1.21 0.00082
-
 pH 6.2, 30°C Rattus norvegicus [2-oxo-3-[(Z)-2-phenylethenyl]quinoxalin-1(2H)-yl]acetic acid
1.1.1.21 0.00087
-
 pH 6.2, 30°C Rattus norvegicus 2-(7-fluoro-3-(4-fluorophenyl)-2-oxoquinoxalin-1(2H)-yl)acetic acid
1.1.1.21 0.00111
-
 pH 6.2, 30°C Rattus norvegicus (3-benzyl-2-oxoquinoxalin-1(2H)-yl)acetic acid
1.1.1.21 0.00152
-
 pH 6.2, 30°C Rattus norvegicus 2-(7-chloro-3-(4-fluorophenyl)-2-oxoquinoxalin-1(2H)-yl)acetic acid
1.1.1.21 0.00213
-
 pH 6.2, 30°C Rattus norvegicus 2-(3,7-bis(4-fluorophenyl)-2-oxoquinoxalin-1(2H)-yl)acetic acid
1.1.1.21 0.00334
-
 pH 6.2, 30°C Rattus norvegicus 2-(7-(4-fluorobenzyl)-3-(2,4-dihydroxyphenyl)-2-oxoquinoxalin-1(2H)-yl)acetic acid
1.1.1.21 0.00338
-
 pH 6.2, 30°C Rattus norvegicus 2-(3-(4-fluorophenyl)-2-oxoquinoxalin-1(2H)-yl)acetic acid
1.1.1.21 0.00418
-
 pH 6.2, 30°C Rattus norvegicus [3-[(E)-2-(4-methoxyphenyl)ethenyl]-2-oxoquinoxalin-1(2H)-yl]acetic acid
1.1.1.21 0.00598
-
 pH 6.2, 30°C Rattus norvegicus 2-(3-phenyl-2-oxoquinoxalin-1(2H)-yl)acetic acid
1.1.1.21 259
-
 pH 6.2, 30°C Rattus norvegicus 2-(3-(4-hydroxyphenyl)-2-oxoquinoxalin-1(2H)-yl)acetic acid

General Information

EC Number General Information Comment Organism
1.1.1.2 metabolism ALR2 is the first rate-determining enzyme in the polyol pathway and catalyzes the reduction of glucose to sorbitol in the presence of NADPH as a cofactor. Sorbitol is in turn converted into fructose with accompanied reduction of NAD+ by sorbitol dehydrogenase. Under normal circumstances, glucose is predominantly converted to glucose-6-phosphate by hexokinase and then enters the glycolytic pathway, whereas only a small amount of glucose is metabolized through the polyol pathway due to a relatively low affinity of ALR2 for this substrate. During hyperglycemia, the polyol metabolic pathway is activated and the increased flux of glucose through the polyol pathway triggers the accumulation of sorbitol, which mainly happens in tissues demonstrating insulin-independent uptake of glucose, such as lens, kidney, retina, and peripheral nerves Rattus norvegicus
1.1.1.21 metabolism ALR2 is the first rate-determining enzyme in the polyol pathway and catalyzes the reduction of glucose to sorbitol in the presence of NADPH as a cofactor. Sorbitol is in turn converted into fructose with accompanied reduction of NAD+ by sorbitol dehydrogenase. Under normal circumstances, glucose is predominantly converted to glucose-6-phosphate by hexokinase and then enters the glycolytic pathway, whereas only a small amount of glucose is metabolized through the polyol pathway due to a relatively low affinity of ALR2 for this substrate. During hyperglycemia, the polyol metabolic pathway is activated and the increased flux of glucose through the polyol pathway triggers the accumulation of sorbitol, which mainly happens in tissues demonstrating insulin-independent uptake of glucose, such as lens, kidney, retina, and peripheral nerves Rattus norvegicus