245116-90-9

245116-90-9 structure

Name: Lidorestat
Chemical Name: 2-[3-[(4,5,7-trifluoro-1,3-benzothiazol-2-yl)methyl]indol-1-yl]acetic acid
CAS Number: 245116-90-9
Molecular Formula: C₁₈H₁₁F₃N₂O₂S
Molecular Weight: 376.35200
Catalog: Signaling Pathways Metabolic Enzyme/Protease Aldose Reductase
Create Date: 2017-01-15 06:44:24
Modify Date: 2024-01-13 18:44:50
Lidorestat (IDD-676) is a potent, selective and orally active aldose reductase inhibitor with an IC50 of 5 nM. Lidorestat can be used to treat chronic diabetes complications. Lidorestat also improves nerve conduction and reduces cataract formation[1][2][3].

Name	2-[3-[(4,5,7-trifluoro-1,3-benzothiazol-2-yl)methyl]indol-1-yl]acetic acid
Synonyms	UNII-R3734K0M7L Lidorestat IDD-676 3NA

Description	Lidorestat (IDD-676) is a potent, selective and orally active aldose reductase inhibitor with an IC50 of 5 nM. Lidorestat can be used to treat chronic diabetes complications. Lidorestat also improves nerve conduction and reduces cataract formation[1][2][3].
Related Catalog	Signaling Pathways >> Metabolic Enzyme/Protease >> Aldose Reductase Research Areas >> Metabolic Disease
Target	IC50: 5 nM (Rldose reductase)[1]
In Vitro	From in vitro experiments, Lidorestat has a reported IC50 against recombinant human aldose reductase (/h/-ALR2) of 5 μM. Against recombinant human aldehyde reductase (/h/-ALR1), Lidorestat has a reported IC50 of 27,000 μM, yielding a selectivity of /h/-ALR1//h/-ALR2 of 5400:1[1][2].
In Vivo	Lidorestat (25 mg/kg/day; oral administration; twice daily; for 6 weeks; diabetic mice) treatment decreases fructose and reduces mortality in diabetic hAR-expressing mice. And Lidorestat does not affect weight[1]. Animal Model: Diabetic low-density lipoprotein (LDL) receptor-deficient [Ldlr(-/-)] mice[1] Dosage: 25 mg/kg/day Administration: Oral administration; twice daily; for 6 weeks Result: Diabetic hAR-expressing mice had decreased fructose and reduced mortality.
References	[1]. Noh HL, et al. Regulation of plasma fructose and mortality in mice by the aldose reductase inhibitor lidorestat. J Pharmacol Exp Ther. 2009 Feb;328(2):496-503. [2]. Van Zandt MC, et al. 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. J Med Chem. 2005 May 5;48(9):3141-52. [3]. Maccari R, et al. Identification of new non-carboxylic acid containing inhibitors of aldose reductase. Bioorg Med Chem. 2010 Jun 1;18(11):4049-55.

Density	1.55g/cm3
Boiling Point	591.4ºC at 760 mmHg
Melting Point	177-178 °C
Molecular Formula	C₁₈H₁₁F₃N₂O₂S
Molecular Weight	376.35200
Flash Point	311.4ºC
Exact Mass	376.04900
PSA	83.36000
LogP	4.34370
Vapour Pressure	7.87E-15mmHg at 25°C
Index of Refraction	1.681
Storage condition	2-8°C