| Identification | Back Directory | [Name]
Fidarestat | [CAS]
136087-85-9 | [Synonyms]
Aldos
Sk 860
CS-489
SNK-860
fidarestat
Fidarestat
(SNK-860
(2S,4S)-6-Fluoro-2',5'-dioxospiro[chroman-4,4'-imidazolidine]-2-carboxamide
(2s,4s)-2-aminoformyl-6-fluoro-spiro[chroman-4,4'-imidazolidine]-2',5'-dione
(2s,4s)-6-fluoro-2',5'-dioxo-2,3-dihydrospiro[chromene-4,4'-imidazolidine]-2-carboxamide
(2S,4S)-2,3-Dihydro-6-fluoro-2',5'-dioxospiro[4H-1-benzopyran-4,4'-imidazolidine]-2-carboxamide
(2S,4S)-6-FLUORO-2'',5''-DIOXOSPIRO(3,4-DIHYDRO-2H-1-BENZOPYRAN-4,4''-IMIDAZOLIDINE)-2-CARBOXAMIDE
Spiro[4H-1-benzopyran-4,4'-imidazolidine]-2-carboxamide, 6-fluoro-2,3-dihydro-2',5'-dioxo-, (2S,4S)-
Spiro(4H-1-benzopyran-4,4'-imidazolidine)-2-carboxamide, 2,3-dihydro-2',5'-dioxo-6-fluoro-, (2S-cis)-
Spiro(4H-1-benzopyran-4,4'-imidazolidine)-2-carboxamide, 6-fluoro-2,3-dihydro-2',5'-dioxo-, (2S-cis)- | [EINECS(EC#)]
200-258-5 | [Molecular Formula]
C12H10FN3O4 | [MDL Number]
MFCD00919183 | [MOL File]
136087-85-9.mol | [Molecular Weight]
279.22 |
| Chemical Properties | Back Directory | [density ]
1.61±0.1 g/cm3(Predicted) | [solubility ]
DMF: 3 mg/ml; DMSO: 5 mg/ml; DMSO:PBS (pH 7.2) (1:1): 0.5 mg/ml; Ethanol: 1 mg/ml | [form ]
A crystalline solid | [pka]
8.46±0.40(Predicted) | [color ]
White to off-white |
| Hazard Information | Back Directory | [Uses]
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. | [Biological Activity]
Fidarestat (SNK 860) is an aldose reductase inhibitor with IC50 values of 26 nM, 33 μM and 1.8 μM for aldose reductase, AKR1B10 and V301L AKR1B10, respectively. Fidarestat (SNK 860) has the potential to study diabetes. | [in vitro]
Fidarestat (SNK-860; 1 or 4 mg/kg. po, daily for 4 weeks) reduces the concentrations of sorbitol and fructose in diabetic rats. | [in vivo]
Fidarestat is an inhibitor of aldose reductase, with IC 50 s of 26 nM, 33 μM, and 1.8 μM for aldose reductase, AKR1B10 and V301L AKR1B10, respectively. | [target]
IC50: 26 nM (Aldose reductase), 33 μM (AKR1B10), 1.8 μM (V301L AKR1B10) | [References]
[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. DOI:10.1016/j.cbi.2012.12.013
[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. DOI:10.1113/expphysiol.1995.sp003909 |
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NCE Biomedical Co.,Ltd.
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LETOPHARM LIMITED
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AFINE CHEMICALS LIMITED
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