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Fidarestat

Names

[ CAS No. ]:
136087-85-9

[ Name ]:
Fidarestat

[Synonym ]:
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

Biological Activity

[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.


[Related Small Molecules]

Isoliquiritigenin | Epalrestat | Ranirestat | Tolrestat | Alrestatin | Aldose reductase-IN-1 | IMIRESTAT | RISARESTAT

Chemical & Physical Properties

[ Density]:
1.6±0.1 g/cm3

[ Molecular Formula ]:
C12H10FN3O4

[ Molecular Weight ]:
279.224

[ Exact Mass ]:
279.065521

[ PSA ]:
110.52000

[ LogP ]:
-0.24

[ Index of Refraction ]:
1.657

Toxicological Information

CHEMICAL IDENTIFICATION

RTECS NUMBER :
WG9863500
CHEMICAL NAME :
Spiro(4H-1-benzopyran-4,4'-imidazolidine)-2-carboxami de, 2,3-dihydro-2',5'-dioxo-6-fluoro-, (2S-cis)-
CAS REGISTRY NUMBER :
136087-85-9
LAST UPDATED :
199712
DATA ITEMS CITED :
3
MOLECULAR FORMULA :
C12-H10-F-N3-O4
MOLECULAR WEIGHT :
279.25

HEALTH HAZARD DATA

ACUTE TOXICITY DATA

TYPE OF TEST :
LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE :
Oral
SPECIES OBSERVED :
Rodent - rat
DOSE/DURATION :
>2 gm/kg
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
TYPE OF TEST :
LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE :
Intravenous
SPECIES OBSERVED :
Rodent - rat
DOSE/DURATION :
1 gm/kg
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
TYPE OF TEST :
LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE :
Oral
SPECIES OBSERVED :
Mammal - dog
DOSE/DURATION :
>2 gm/kg
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

Related Compounds