TOLRESTAT

TOLRESTAT Basic information
Product Name:TOLRESTAT
Synonyms:TOLRESTAT;TOLRESTAT(FORR&DONLY);Alredase;AY-27773;Lorestat;N-[[6-Methoxy-5-(triiquoromethyl)-1-naphthalenyl]thioxomethyl]-N-methylglyeine;Aldredase;N-[[6-Methoxy-5-(trifluoromethyl)naphthalen-1-yl]thioxomethyl]-N-methylglycine
CAS:82964-04-3
MF:C16H14F3NO3S
MW:357.35
EINECS:
Product Categories:
Mol File:82964-04-3.mol
TOLRESTAT Structure
TOLRESTAT Chemical Properties
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)
pka3.49±0.10(Predicted)
form powder
color white to beige
CAS DataBase Reference82964-04-3
Safety Information
MSDS Information
TOLRESTAT Usage And Synthesis
DescriptionTolrestat is a long-acting aldose reductase inhibitor reportedly useful in the prophylaxis of diabetic neuropathy, retinopathy and cataracts.
DescriptionTolrestat 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.
OriginatorAmerican Home Products (USA)
UsesTolrestat is an aldose reductase inhibitor.
UsesAlredase (Wyeth-Ayerst).
DefinitionChEBI: Tolrestat is a member of naphthalenes. It has a role as an EC 1.1.1.21 (aldehyde reductase) inhibitor.
Brand nameAlredase
Biochem/physiol ActionsTolrestat 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.
TOLRESTAT Preparation Products And Raw materials
Raw materialsPhosphorus pentasulfide-->Glycine methyl ester hydrochloride-->Sarcosine-->1-Naphthoic acid-->1,5-DIMETHYLNAPHTHALENE
Oxalic acid dihydrate Acetonitrile Naphthalene Benzyl alcohol Stearic acid Naftifine Anthracene alpha,alpha,alpha-Trifluoro-o-cresol TOLRESTAT 1-TRIFLUOROMETHYL-NAPHTHALENE N-methylthiobenzamide Tolrestat S-oxide 2-(TRIFLUOROMETHYL)ANISOLE

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