136087-85-9

Basic information

• Product Name: Fidarestat
• Synonyms: (2s,4s)-6-fluoro-2',5'-dioxo-2,3-dihydrospiro[chromene-4,4'-imidazolidine]-2-carboxamide;(2s,4s)-2-aminoformyl-6-fluoro-spiro[chroman-4,4'-imidazolidine]-2',5'-dione;fidarestat;(2S,4S)-6-FLUORO-2'',5''-DIOXOSPIRO(3,4-DIHYDRO-2H-1-BENZOPYRAN-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;SNK-860;Aldos
• CAS NO: 136087-85-9
• Molecular Formula: C12H10FN3O4
• Molecular Weight: 279.22
• EINECS: 200-258-5
• Mol File: 136087-85-9.mol
• Article Data: 7

Chemical Properties

• Appearance: /
• Density: 1.616 g/cm³
• Refractive Index: 1.657
• PKA: 8.46±0.40(Predicted)
• CAS DataBase Reference: Fidarestat(CAS DataBase Reference)
• NIST Chemistry Reference: Fidarestat(136087-85-9)
• EPA Substance Registry System: Fidarestat(136087-85-9)

Safety Data

• Hazardous Substances Data: 136087-85-9(Hazardous Substances Data)

Usage

Description

Fidarestat is an aldose reductase inhibitor (ARI), a type of drug that is primarily used for the management of diabetic neuropathy, a common complication of diabetes. It functions by blocking the action of the aldose reductase enzyme, which is involved in the metabolism of glucose. The inhibition of this enzyme can help prevent or slow down nerve damage in individuals with diabetes. Fidarestat is still in clinical development and has not been approved for general use by regulatory authorities. It is under investigation due to its potential in alleviating symptoms and complications of chronic diabetes.

Uses

Used in Pharmaceutical Industry:
Fidarestat is used as a therapeutic agent for the management of diabetic neuropathy, aiming to prevent or slow down nerve damage in individuals with diabetes.
Used in Clinical Research:
Fidarestat is used as a subject of investigation in clinical trials, with the goal of evaluating its potential in alleviating symptoms and complications of chronic diabetes.

InChI:InChI=1/C12H10FN3O4/c13-5-1-2-7-6(3-5)12(4-8(20-7)9(14)17)10(18)15-11(19)16-12/h1-3,8H,4H2,(H2,14,17)(H2,15,16,18,19)/t8-,12-/m0/s1

Upstream product

• 116925-74-7 dl-6-fluoro-2,3-dihydro-2',5'-dioxo-spiro[4H-1-benzopyran-4,4'-imidazolidine]-2-carboxylic acid 
• 105300-40-1 (+)-6-fluoro-3,4-dihydro-4-oxo-2H-1-benzopyran-2-carboxylic acid 
• 118803-65-9 (E)-4-(5-fluoro-2-hydroxyphenyl)-4-oxo-2-butenoic acid 
• 459-60-9 1-fluoro-4-methoxybenzene 
• 118803-67-1 (2S)-6-fluoro-3,4-dihydro-4-oxo-N-((S)-1-phenylethyl)-2H-1-benzopyran-2-carboxamide 
• 136087-84-8 (2S,4S)-(+)-6-fluoro-2,3-dihydro-2',5'-dioxospiro<4H-1-benzopyran-4,4'-imidazolidine>-2-carboxylic acid 
• 118803-69-3 (2S)-6-fluoro-3,4-dihydro-4-oxo-2H-1-benzopyran-2-carboxylic acid 
• 118803-66-0 (+/-)-6-fluoro-3,4-dihydro-4-oxo-2H-1-benzopyran-2-carbonyl chloride 
• 136087-83-7 (2S,4S)-6-Fluoro-2',5'-dioxospiro[chroman-4,4'-imidazolidine]-2-carboxylic acid 2-propyl ester 
• 118803-68-2 (2R)-6-fluoro-3,4-dihydro-4-oxo-N-((S)-1-phenylethyl)-2H-1-benzopyran-2-carboxamide 
• 159574-05-7 (2R,4S)-(-)-6-fluoro-2,3-dihydro-2',5'-dioxospiro<4H-1-benzopyran-4,4'-imidazolidine>-2-carboxylic acid 
• 118803-70-6 (2R)-6-fluoro-3,4-dihydro-4-oxo-2H-1-benzopyran-2-carboxylic acid 
• 159574-09-1 (2R,4S)-6-fluoro-2,3-dihydro-2',5'-dioxospiro<4H-1-benzopyran-4,4'-imidazolidine>-2-carboxylic acid n-propyl ester 
• 159574-03-5 (2S,4R)-(+)-6-fluoro-2,3-dihydro-2',5'-dioxospiro<4H-1-benzopyran-4,4'-imidazolidine>-2-carboxylic acid 

Related news

Erythrocytic sorbitol contents in diabetic patients correlate with blood aldose reductase protein contents and plasma glucose levels, and are normalized by the potent aldose reductase inhibitor Fidarestat (cas 136087-85-9) (SNK-860)09/05/2019

The accumulation of sorbitol by the activated polyol pathway is considered to be a major cause of diabetic neuropathy. Because the erythrocytic sorbitol contents reportedly reflects that in nerves, erythrocytic sorbitol measurement would be useful for confirming the effect of an aldose reductase...detailed

Effects of 15-month aldose reductase inhibition with Fidarestat (cas 136087-85-9) on the experimental diabetic neuropathy in rats09/04/2019

We examined the effects of long-term treatment with an aldose reductase inhibitor (ARI) fidarestat on functional, morphological and metabolic changes in the peripheral nerve of 15-month diabetic rats induced by streptozotocin (STZ). Slowed F-wave, motor nerve and sensory nerve conduction velocit...detailed

Long-term treatment with Fidarestat (cas 136087-85-9) suppresses the development of diabetic retinopathy in STZ-induced diabetic rats09/03/2019

It is important to suppress retinal vascular changes for prevention of the onset and progression of diabetic retinopathy. In the present study, we investigated the dose–response effect of an aldose reductase (AR) inhibitor, fidarestat, on retinal vascular changes in the retinas of streptozotoci...detailed

Fidarestat (cas 136087-85-9) (SNK-860), a potent aldose reductase inhibitor, normalizes the elevated sorbitol accumulation in erythrocytes of diabetic patients09/01/2019

Sorbitol accumulation in nerves has been regarded as one of the major causes of diabetic neuropathy. In this study, fidarestat (SNK-860; 1 mg daily), a potent new aldose reductase inhibitor (ARI), or the commercially available ARI epalrestat (150 mg daily), was administered for 4 weeks to 58 Typ...detailed

Plasma protein binding, pharmacokinetics, tissue distribution and CYP450 biotransformation studies of Fidarestat (cas 136087-85-9) by ultra high performance liquid chromatography–high resolution mass spectrometry08/31/2019

Fidarestat, an aldose reductase inhibitor, has been used for the treatment of the diabetic associated complications such as retinopathy, neuropathy and nephropathy. To better understand the metabolism and pharmacokinetics of fidarestat, we have evaluated plasma protein binding, pharmacokinetics,...detailed

Original ArticleAldose reductase inhibitor, Fidarestat (cas 136087-85-9) regulates mitochondrial biogenesis via Nrf2/HO-1/AMPK pathway in colon cancer cells08/29/2019

Although we have shown earlier that aldose reductase (AR) inhibitors prevent colorectal cancer cell (CRC) growth in culture as well as in nude mice xenografts, the mechanism(s) is not well understood. In this study, we have investigated how AR inhibition prevents CRC growth by regulating the mit...detailed

Aldose reductase inhibitor, Fidarestat (cas 136087-85-9) prevents doxorubicin-induced endothelial cell death and dysfunction08/28/2019

Despite doxorubicin (Dox) being one of the most widely used chemotherapy agents for breast, blood and lung cancers, its use in colon cancer is limited due to increased drug resistance and severe cardiotoxic side effects that increase mortality associated with its use at high doses. Therefore, be...detailed

Relevant articles and documents

USE OF SUBSTITUTED 2 PHENYLBENZIMIDAZOLES AS MEDICAMENTS

The present invention relates to the use of a substituted 2-phenylbenzimidazole of formula I wherein R1, R2, R3, R 4, R5 and m have the meanings given in the claims, for the preparation of a medicament for the treatment or prevention of diseases involving glucagon receptors, as well as new compounds of formula I wherein R1 is a group of formula

Hydantoin derivatives for treating complications of diabetes

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Spiro-3-heteroazolidine compounds and salts thereof, their preparation and pharmaceutical agents thereof

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