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Literature summary extracted from

  • Rakowitz, D.; Maccari, R.; Ottana, R.; Vigorita, M.G.
    In vitro aldose reductase inhibitory activity of 5-benzyl-2,4-thiazolidinediones (2006), Bioorg. Med. Chem., 14, 567-574.
    View publication on PubMed

Inhibitors

EC Number Inhibitors Comment Organism Structure
1.1.1.21 (5-biphenyl-4-ylmethyl-2,4-dioxothiazolidin-3-yl)acetic acid IC50: 0.0017 mM Bos taurus
1.1.1.21 (5-biphenyl-4-ylmethyl-2,4-dioxothiazolidin-3-yl)acetic acid methyl ester 15% inhibition of ALR2 at 0.05 mM Bos taurus
1.1.1.21 5-(3-methoxybenzyl)-2,4-thiazolidinedione 16% inhibition of ALR2 at 0.05 mM Bos taurus
1.1.1.21 5-(3-phenoxybenzyl)-2,4-thiazolidinedione IC50: 0.0789 mM Bos taurus
1.1.1.21 5-(4-benzyloxybenzyl)-2,4-thiazolidinedione IC50: 0.0314 mM Bos taurus
1.1.1.21 5-(4-methoxybenzyl)-2,4-thiazolidinedione 21% inhibition of ALR2 at 0.05 mM Bos taurus
1.1.1.21 5-(4-phenoxybenzyl)-2,4-thiazolidinedione IC50: 0.0404 mM Bos taurus
1.1.1.21 5-biphenyl-4-ylmethyl-2,4-thiazolidinedione IC50: 0.0658 mM Bos taurus
1.1.1.21 epalrestat
-
Bos taurus
1.1.1.21 additional information poor inhibition by [2,4-dioxo-5-(4-phenoxybenzyl)thiazolidin-3-yl]acetic acid methyl ester Bos taurus
1.1.1.21 pioglitazone
-
Bos taurus
1.1.1.21 ponalrestat IC50: 80 nM Bos taurus
1.1.1.21 rosiglitazone
-
Bos taurus
1.1.1.21 sorbinil IC50: 0.0034 mM Bos taurus
1.1.1.21 [2,4-dioxo-5-(3-phenoxybenzyl)thiazolidin-3-yl]acetic acid IC50: 0.0010 mM Bos taurus
1.1.1.21 [2,4-dioxo-5-(3-phenoxybenzyl)thiazolidin-3-yl]acetic acid methyl ester 26% inhibition of ALR2 at 0.05 mM Bos taurus
1.1.1.21 [2,4-dioxo-5-(4-phenoxybenzyl)thiazolidin-3-yl]acetic acid IC50: 0.0028 mM Bos taurus
1.1.1.21 [5-(3-methoxybenzyl)-2,4-dioxothiazolidin-3-yl]acetic acid IC50: 0.0030 mM Bos taurus
1.1.1.21 [5-(3-methoxybenzyl)-2,4-dioxothiazolidin-3-yl]acetic acid methyl ester IC50: 0.0211 mM Bos taurus
1.1.1.21 [5-(4-benzyloxybenzyl)-2,4-dioxothiazolidin-3-yl]acetic acid methyl ester 24% inhibition of ALR2 at 0.05 mM Bos taurus
1.1.1.21 [5-(4-hydroxybenzyl)-2,4-dioxothiazolidin-3-yl]acetic acid IC50: 0.0021 mM Bos taurus
1.1.1.21 [5-(4-methoxybenzyl)-2,4-dioxothiazolidin-3-yl]acetic acid IC50: 0.0011 mM Bos taurus
1.1.1.21 [5-(4-methoxybenzyl)-2,4-dioxothiazolidin-3-yl]acetic acid methyl ester 24% inhibition of ALR2 at 0.05 mM Bos taurus

Organism

EC Number Organism UniProt Comment Textmining
1.1.1.21 Bos taurus
-
-
-

Source Tissue

EC Number Source Tissue Comment Organism Textmining
1.1.1.21 lens
-
Bos taurus
-

Substrates and Products (Substrate)

EC Number Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
1.1.1.21 glyceraldehyde + NADPH + H+
-
Bos taurus glycerol + NADP+
-
?

Synonyms

EC Number Synonyms Comment Organism
1.1.1.21 aldose reductase
-
Bos taurus
1.1.1.21 ALR2
-
Bos taurus

Temperature Optimum [°C]

EC Number Temperature Optimum [°C] Temperature Optimum Maximum [°C] Comment Organism
1.1.1.21 37
-
assay at Bos taurus

pH Optimum

EC Number pH Optimum Minimum pH Optimum Maximum Comment Organism
1.1.1.21 7
-
assay at Bos taurus

Cofactor

EC Number Cofactor Comment Organism Structure
1.1.1.21 NADPH
-
Bos taurus

IC50 Value

EC Number IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
1.1.1.21 0.00008
-
IC50: 80 nM Bos taurus ponalrestat
1.1.1.21 0.001
-
IC50: 0.0010 mM Bos taurus [2,4-dioxo-5-(3-phenoxybenzyl)thiazolidin-3-yl]acetic acid
1.1.1.21 0.0011
-
IC50: 0.0011 mM Bos taurus [5-(4-methoxybenzyl)-2,4-dioxothiazolidin-3-yl]acetic acid
1.1.1.21 0.0017
-
IC50: 0.0017 mM Bos taurus (5-biphenyl-4-ylmethyl-2,4-dioxothiazolidin-3-yl)acetic acid
1.1.1.21 0.0021
-
IC50: 0.0021 mM Bos taurus [5-(4-hydroxybenzyl)-2,4-dioxothiazolidin-3-yl]acetic acid
1.1.1.21 0.0028
-
IC50: 0.0028 mM Bos taurus [2,4-dioxo-5-(4-phenoxybenzyl)thiazolidin-3-yl]acetic acid
1.1.1.21 0.003
-
IC50: 0.0030 mM Bos taurus [5-(3-methoxybenzyl)-2,4-dioxothiazolidin-3-yl]acetic acid
1.1.1.21 0.0034
-
IC50: 0.0034 mM Bos taurus sorbinil
1.1.1.21 0.0211
-
IC50: 0.0211 mM Bos taurus [5-(3-methoxybenzyl)-2,4-dioxothiazolidin-3-yl]acetic acid methyl ester
1.1.1.21 0.0314
-
IC50: 0.0314 mM Bos taurus 5-(4-benzyloxybenzyl)-2,4-thiazolidinedione
1.1.1.21 0.0404
-
IC50: 0.0404 mM Bos taurus 5-(4-phenoxybenzyl)-2,4-thiazolidinedione
1.1.1.21 0.0658
-
IC50: 0.0658 mM Bos taurus 5-biphenyl-4-ylmethyl-2,4-thiazolidinedione
1.1.1.21 0.0789
-
IC50: 0.0789 mM Bos taurus 5-(3-phenoxybenzyl)-2,4-thiazolidinedione