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HomeProduct name listTOLRESTAT

TOLRESTAT

Synonym(s):AY-27773;CID 53359;N-[[5 -(Trifluoromethyl)-6-methoxy-lnaphthalenyl]thioxomethyl]-N-methylglycine;N-[[6-Methoxy-5-(trifluoromethyl)-1-naphthalenyl]thioxomethyl]-N-methyl-glycine;Tolrestatin

TOLRESTAT Structural

What is TOLRESTAT?

Description

Tolrestat is a long-acting aldose reductase inhibitor reportedly useful in the prophylaxis of diabetic neuropathy, retinopathy and cataracts.

Description

Tolrestat is an aldose reductase inhibitor (IC50 = 35 nM for the bovine lens enzyme). Dietary administration of tolrestat decreases sciatic nerve galactitol accumulation in a rat model of galactosemia (ED50 = 7.3 mg/kg per day) and sciatic nerve sorbitol accumulation (ED50 = 4.8 mg/kg per day) in a rat model of diabetes induced by streptozotocin (STZ; ). It also decreases urinary total protein exretion in a rat model of STZ-induced diabetes when administered at a dose of 25 mg/kg per day. Topical administration of tolrestat (2 and 3% in 10 μl four times per day) decreases levels of galactitol in the lens of and inhibits cataract formation in rats fed a high-galactose diet.

Originator

American Home Products (USA)

The Uses of TOLRESTAT

Tolrestat is an aldose reductase inhibitor.

The Uses of TOLRESTAT

Alredase (Wyeth-Ayerst).

Definition

ChEBI: Tolrestat is a member of naphthalenes. It has a role as an EC 1.1.1.21 (aldehyde reductase) inhibitor.

brand name

Alredase

Biochem/physiol Actions

Tolrestat is considered to be effective in treating the consequences of diabetes including neuropathy, nephropathy, retinopathy and esophageal motility and vibration perception. Tolrestat is also believed to have lesser or no toxic effects.

Properties of TOLRESTAT

Melting point: 164-165°
Boiling point: 498.1±55.0 °C(Predicted)
Density  1.399±0.06 g/cm3(Predicted)
storage temp.  2-8°C
solubility  Chloroform (Slightly), DMSO (Slightly), Ethyl Acetate (Slightly)
pka 3.49±0.10(Predicted)
form  powder
color  white to beige
CAS DataBase Reference 82964-04-3

Safety information for TOLRESTAT

Signal word Warning
Pictogram(s)
ghs
Exclamation Mark
Irritant
GHS07
GHS Hazard Statements H302:Acute toxicity,oral
H315:Skin corrosion/irritation
H319:Serious eye damage/eye irritation
H332:Acute toxicity,inhalation
H335:Specific target organ toxicity, single exposure;Respiratory tract irritation
Precautionary Statement Codes P261:Avoid breathing dust/fume/gas/mist/vapours/spray.
P280:Wear protective gloves/protective clothing/eye protection/face protection.
P305+P351+P338:IF IN EYES: Rinse cautiously with water for several minutes. Remove contact lenses, if present and easy to do. Continuerinsing.

Computed Descriptors for TOLRESTAT

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