| Bioactivity | Fidarestat (SNK 860) is an inhibitor of aldose reductase, with IC50s of 26 nM, 33 μM, and 1.8 μM for aldose reductase, AKR1B10 and V301L AKR1B10, respectively; Fidarestat (SNK 860) has the potential to treat diabetic disease. | |||||||||
| Target | IC50: 26 nM (Aldose reductase), 33 μM (AKR1B10), 1.8 μM (V301L AKR1B10) | |||||||||
| Invitro | Fidarestat is an inhibitor of aldose reductase, with IC50s of 26 nM, 33 μM, and 1.8 μM for aldose reductase, AKR1B10 and V301L AKR1B10, respectively[1]. | |||||||||
| In Vivo | Fidarestat (SNK-860; 1 or 4 mg/kg. p.o., daily for 4 weeks) reduces the concentrations of sorbitol and fructose in diabetic rats[2]. | |||||||||
| Name | Fidarestat | |||||||||
| CAS | 136087-85-9 | |||||||||
| Formula | C12H10FN3O4 | |||||||||
| Molar Mass | 279.22 | |||||||||
| Appearance | Solid | |||||||||
| Transport | Room temperature in continental US; may vary elsewhere. | |||||||||
| Storage |
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| Reference | [1]. Ruiz FX, et al. X-ray structure of the V301L aldo-keto reductase 1B10 complexed with NADP(+) and the potent aldose reductase inhibitor fidarestat: implications for inhibitor binding and selectivity. Chem Biol Interact. 2013 Feb 25;202(1-3):178-85. [2]. Hotta N, et al. Effect of an aldose reductase inhibitor, SNK-860, on deficits in the electroretinogram of diabetic rats. Exp Physiol. 1995 Nov;80(6):981-9. |