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Lidorestat

Names

[ CAS No. ]:
245116-90-9

[ Name ]:
Lidorestat

[Synonym ]:
UNII-R3734K0M7L
Lidorestat
IDD-676
3NA

Biological Activity

[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.

Chemical & Physical Properties

[ 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

Related Compounds