Details
Stereochemistry | ACHIRAL |
Molecular Formula | C18H11F3N2O2S.H2O |
Molecular Weight | 394.368 |
Optical Activity | NONE |
Defined Stereocenters | 0 / 0 |
E/Z Centers | 0 |
Charge | 0 |
SHOW SMILES / InChI
SMILES
O.OC(=O)CN1C=C(CC2=NC3=C(S2)C(F)=CC(F)=C3F)C4=C1C=CC=C4
InChI
InChIKey=DLZGQGBHYCAKQA-UHFFFAOYSA-N
InChI=1S/C18H11F3N2O2S.H2O/c19-11-6-12(20)18-17(16(11)21)22-14(26-18)5-9-7-23(8-15(24)25)13-4-2-1-3-10(9)13;/h1-4,6-7H,5,8H2,(H,24,25);1H2
Molecular Formula | C18H11F3N2O2S |
Molecular Weight | 376.352 |
Charge | 0 |
Count |
|
Stereochemistry | ACHIRAL |
Additional Stereochemistry | No |
Defined Stereocenters | 0 / 0 |
E/Z Centers | 0 |
Optical Activity | NONE |
Molecular Formula | H2O |
Molecular Weight | 18.0153 |
Charge | 0 |
Count |
|
Stereochemistry | ACHIRAL |
Additional Stereochemistry | No |
Defined Stereocenters | 0 / 0 |
E/Z Centers | 0 |
Optical Activity | NONE |
Lidorestat is a highly potent and selective aldose reductase inhibitor with good oral bioavailability that is reported to improve nerve conduction and reduce cataract formation. Lidorestat reduced mortality rates in hAR transgenic mice. Mice receiving lidorestat had similar survival rates as nonhAR-expressing diabetic mice. Lidorestat treatment did not affect plasma lipids, glucose, or weights of diabetic mice. Drugs such as lidorestat will improve human health by reducing the production of toxic products of the polyol pathway. Lidorestat was developed for the treatment of diabetic complications, including neuropathy, retinopathy, cataracts, nephropathy.
Approval Year
PubMed
Title | Date | PubMed |
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Prevention of sensory disorders in diabetic Sprague-Dawley rats by aldose reductase inhibition or treatment with ciliary neurotrophic factor. | 2004 Apr |
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Role of aldose reductase and oxidative damage in diabetes and the consequent potential for therapeutic options. | 2005 May |
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Discovery of [3-(4,5,7-trifluoro-benzothiazol-2-ylmethyl)-pyrrolo[2,3-b]pyridin-1-yl]acetic acids as highly potent and selective inhibitors of aldose reductase for treatment of chronic diabetic complications. | 2009 Apr 1 |
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Diabetic cataract-pathogenesis, epidemiology and treatment. | 2010 |
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Identification of new non-carboxylic acid containing inhibitors of aldose reductase. | 2010 Jun 1 |
|
High glucose concentration suppresses a SIRT2 regulated pathway that enhances neurite outgrowth in cultured adult sensory neurons. | 2018 Nov |
Sample Use Guides
In Vivo Use Guide
Sources: https://www.ncbi.nlm.nih.gov/pubmed/18974362
Curator's Comment: Mice data
25 mg/kg/day for 6 weeks
Route of Administration:
Oral
Substance Class |
Chemical
Created
by
admin
on
Edited
Fri Dec 15 15:51:18 GMT 2023
by
admin
on
Fri Dec 15 15:51:18 GMT 2023
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Record UNII |
9Z74BD3QPP
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Record Status |
Validated (UNII)
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Record Version |
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C72880
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CHEMBL363387
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C72815
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C500848
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Related Record | Type | Details | ||
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PARENT -> SALT/SOLVATE | |||
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ANHYDROUS->SOLVATE |
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ACTIVE MOIETY |