Fidarestat

Modify Date: 2024-01-06 21:32:11

Fidarestat Structure
Fidarestat structure
 Common Name Fidarestat
CAS Number 136087-85-9 Molecular Weight 279.224
Density 1.6±0.1 g/cm3 Boiling Point N/A
Molecular Formula C12H10FN3O4 Melting Point N/A
MSDS N/A Flash Point N/A

 Use of Fidarestat


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.

 Names

Name Fidarestat
Synonym More Synonyms

 Fidarestat 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
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 & 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

 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
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