| Bioactivity | Lidorestat (IDD-676) is a potent, selective and orally active aldose reductase inhibitor with an IC50 of 5 nM. Lidorestat can be used for chronic diabetes complications. Lidorestat also improves nerve conduction and reduces cataract formation[1][2][3]. | ||||||||||||
| Target | IC50: 5 nM (Rldose reductase) | ||||||||||||
| Invitro | 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: | ||||||||||||
| Name | Lidorestat | ||||||||||||
| CAS | 245116-90-9 | ||||||||||||
| Formula | C18H11F3N2O2S | ||||||||||||
| Molar Mass | 376.35 | ||||||||||||
| Appearance | Solid | ||||||||||||
| Transport | Room temperature in continental US; may vary elsewhere. | ||||||||||||
| Storage |
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| Reference | [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 M [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. |
Lidorestat
CAS: 245116-90-9 F: C18H11F3N2O2S W: 376.35
Lidorestat (IDD-676) is a potent, selective and orally active aldose reductase inhibitor with an IC50 of 5 nM. Lidoresta
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