136087-85-9

136087-85-9 structure

Name: Fidarestat
Chemical Name: Fidarestat
CAS Number: 136087-85-9
Molecular Formula: C₁₂H₁₀FN₃O₄
Molecular Weight: 279.224
Catalog: Signaling Pathways Metabolic Enzyme/Protease Aldose Reductase
Create Date: 2018-05-21 08:00:00
Modify Date: 2024-01-06 21:32:11
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.

Name	Fidarestat
Synonyms	SNK-860 Fidarestat (+)-(2S,4S)-6-Fluoro-2',5'-dioxo-2,3-dihydrospiro[chromene-4,4'-imidazolidine]-2-carboxamide Spiro(4H-1-benzopyran-4,4'-imidazolidine)-2-carboxamide,6-fluoro-2,3-dihydro-2',5'-dioxo-,(2S-cis) (2s,4s)-2-aminoformyl-6-fluoro-spiro[chroman-4,4'-imidazolidine]-2',5'-dione Spiro[4H-1-benzopyran-4,4'-imidazolidine]-2-carboxamide, 6-fluoro-2,3-dihydro-2',5'-dioxo-, (2S,4S)- (2S,4S)-6-Fluoro-2',5'-dioxospiro[chroman-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[chroman-4,4'-imidazolidine]-2-carboxamide (2S,4S)-6-Fluoro-2',5'-dioxo-2,3-dihydrospiro[chromene-4,4'-imidazolidine]-2-carboxamide (2S,4S)-6-FLUORO-2'',5''-DIOXOSPIRO(3,4-DIHYDRO-2H-1-BENZOPYRAN-4,4''-IMIDAZOLIDINE)-2-CARBOXAMIDE Aldos Sk 860

Description	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.
Related Catalog	Signaling Pathways >> Metabolic Enzyme/Protease >> Aldose Reductase Research Areas >> Metabolic Disease
Target	IC50: 26 nM (Aldose reductase), 33 μM (AKR1B10), 1.8 μM (V301L AKR1B10)[1]
In Vitro	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].
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. [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.

CHEMICAL NAME :: Spiro(4H-1-benzopyran-4,4'-imidazolidine)-2-carboxami de, 2,3-dihydro-2',5'-dioxo-6-fluoro-, (2S-cis)-

TOXIC EFFECTS :: Details of toxic effects not reported other than lethal dose value

REFERENCE :: EXMDA4 International Congress Series--Excerpta Medica. (Excerpta Medica, Inc., POB 3085, Princeton, NJ 08540) No.1- 1952- Volume(issue)/page/year: 913,89,1990

TOXIC EFFECTS :: Details of toxic effects not reported other than lethal dose value

REFERENCE :: EXMDA4 International Congress Series--Excerpta Medica. (Excerpta Medica, Inc., POB 3085, Princeton, NJ 08540) No.1- 1952- Volume(issue)/page/year: 913,89,1990

TOXIC EFFECTS :: Details of toxic effects not reported other than lethal dose value

REFERENCE :: EXMDA4 International Congress Series--Excerpta Medica. (Excerpta Medica, Inc., POB 3085, Princeton, NJ 08540) No.1- 1952- Volume(issue)/page/year: 913,89,1990