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Details

Stereochemistry ACHIRAL
Molecular Formula C18H11F3N2O2S
Molecular Weight 376.352
Optical Activity NONE
Defined Stereocenters 0 / 0
E/Z Centers 0
Charge 0

SHOW SMILES / InChI
Structure of LIDORESTAT ANHYDROUS

SMILES

OC(=O)CN1C=C(CC2=NC3=C(F)C(F)=CC(F)=C3S2)C4=C1C=CC=C4

InChI

InChIKey=KYHVTMFADJNSGS-UHFFFAOYSA-N
InChI=1S/C18H11F3N2O2S/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)

HIDE SMILES / InChI

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

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

PubMed

TitleDatePubMed
High glucose concentration suppresses a SIRT2 regulated pathway that enhances neurite outgrowth in cultured adult sensory neurons.
2018-11
Updates on Aldose Reductase Inhibitors for Management of Diabetic Complications and Non-diabetic Diseases.
2016
[5-(Benzyloxy)-1H-indol-1-yl]acetic acid, an aldose reductase inhibitor and PPARγ ligand.
2015
Identification of new non-carboxylic acid containing inhibitors of aldose reductase.
2010-06-01
Diabetic cataract-pathogenesis, epidemiology and treatment.
2010
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.
2009-04-01
Regulation of plasma fructose and mortality in mice by the aldose reductase inhibitor lidorestat.
2009-02
Synthesis, induced-fit docking investigations, and in vitro aldose reductase inhibitory activity of non-carboxylic acid containing 2,4-thiazolidinedione derivatives.
2008-06-01
Discovery of 3-[(4,5,7-trifluorobenzothiazol-2-yl)methyl]indole-N-acetic acid (lidorestat) and congeners as highly potent and selective inhibitors of aldose reductase for treatment of chronic diabetic complications.
2005-05-05
Role of aldose reductase and oxidative damage in diabetes and the consequent potential for therapeutic options.
2005-05
Prevention of sensory disorders in diabetic Sprague-Dawley rats by aldose reductase inhibition or treatment with ciliary neurotrophic factor.
2004-04

Sample Use Guides

In Vivo Use Guide
Curator's Comment: Mice data
25 mg/kg/day for 6 weeks
Route of Administration: Oral
Substance Class Chemical
Created
by admin
on Mon Mar 31 18:20:39 GMT 2025
Edited
by admin
on Mon Mar 31 18:20:39 GMT 2025
Record UNII
R3734K0M7L
Record Status Validated (UNII)
Record Version
  • Download
Name Type Language
IDD-000676
Preferred Name English
LIDORESTAT ANHYDROUS
Common Name English
lidorestat [INN]
Common Name English
(3-((4,5,7-TRIFLUORO-1,3-BENZOTHIAZOL-2-YL)METHYL)-1H-INDOL-1-YL)ACETIC ACID
Systematic Name English
1H-INDOLE-1-ACETIC ACID, 3-((4,5,7-TRIFLUORO-2-BENZOTHIAZOLYL)METHYL)-
Common Name English
Classification Tree Code System Code
NCI_THESAURUS C72880
Created by admin on Mon Mar 31 18:20:39 GMT 2025 , Edited by admin on Mon Mar 31 18:20:39 GMT 2025
Code System Code Type Description
CAS
245116-90-9
Created by admin on Mon Mar 31 18:20:39 GMT 2025 , Edited by admin on Mon Mar 31 18:20:39 GMT 2025
PRIMARY
NCI_THESAURUS
C81356
Created by admin on Mon Mar 31 18:20:39 GMT 2025 , Edited by admin on Mon Mar 31 18:20:39 GMT 2025
PRIMARY
PUBCHEM
157839
Created by admin on Mon Mar 31 18:20:39 GMT 2025 , Edited by admin on Mon Mar 31 18:20:39 GMT 2025
PRIMARY
INN
8162
Created by admin on Mon Mar 31 18:20:39 GMT 2025 , Edited by admin on Mon Mar 31 18:20:39 GMT 2025
PRIMARY
FDA UNII
R3734K0M7L
Created by admin on Mon Mar 31 18:20:39 GMT 2025 , Edited by admin on Mon Mar 31 18:20:39 GMT 2025
PRIMARY
SMS_ID
100000176280
Created by admin on Mon Mar 31 18:20:39 GMT 2025 , Edited by admin on Mon Mar 31 18:20:39 GMT 2025
PRIMARY
EPA CompTox
DTXSID40179264
Created by admin on Mon Mar 31 18:20:39 GMT 2025 , Edited by admin on Mon Mar 31 18:20:39 GMT 2025
PRIMARY
Related Record Type Details
SALT/SOLVATE -> PARENT
TARGET -> INHIBITOR
SOLVATE->ANHYDROUS
Related Record Type Details
ACTIVE MOIETY