AY-27773 MedChemExpress (MCE)

Product Name	TOLRESTAT
Synonyms	Lorestat AY-27773 Alredase Aldredase TOLRESTAT N-[[6-Methoxy-5-(triiquoromethyl)-1-naphthalenyl]thioxomethyl]-N-methylglyeine N-[[6-Methoxy-5-(trifluoromethyl)naphthalen-1-yl]thioxomethyl]-N-methylglycine
CAS	82964-04-3
EINECS
Chemical Formula	C16H14F3NO3S
Molecular Weight	357.35
inchi
Package	10 mM * 1 mL;1 mg;5 mg;10 mg;25 mg;50 mg
Price	Email to quote
Descriptions	Tolrestat Tolrestat MedChemExpress (MCE) HY-16500 82964-04-3 AY-27773 99.37% Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year Room temperature in continental US Descriptions Tolrestat Tolrestat MedChemExpress (MCE) HY-16500 82964-04-3 AY-27773 99.37% Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year Room temperature in continental US may vary elsewhere. Tolrestat is a potent, orally active aldose reductase inhibitor with IC50 of 35 nM. Tolrestat (1.8 mg/kg per day) causes a reversal to normal RBC sorbitol levels diabetic rats[1]. In 21-day diabetic rats, the estimated ID in the sciatic nerve and lenses is 4.8 and about 20 for tolrestat, and 1.7 and 2.2 for (±)sorbinil,respectively[2]. Either tolrestat or sorbinil inhibits tissue AR activity but does not significantly affect plasma lipoprotein levels, or affect the body weight of the mice or their general health. Accumulation of cholesterol-rich foam cells is significantly increased in aortic roots of tolrestat-fed mice[3]. For a period of four days, rats weighing about 70 g are given unlimited access to water and Chow supplemented with 20% (wt/wt) galactose and tolrestat at various dose levels. Rats used as control receive chow containing galactose (20%, wt/wt) or glucose (20%, wt/wt). The rats are killed the lenses and sciatic nerves are removed and homogenized in 5% trichloroacetic acid the deproteinized extracts are then analyzed for galactitol by a modification of a method for glycerol determination. The values obtained in the group fed 20% glucose are used for background correction. IC50: 35 nM (Aldose Reductase) In Vivo Tolrestat (1.8 mg/kg per day) causes a reversal to normal RBC sorbitol levels diabetic rats[1]. In 21-day diabetic rats, the estimated ID in the sciatic nerve and lenses is 4.8 and about 20 for tolrestat, and 1.7 and 2.2 for (±)sorbinil,respectively[2]. Either tolrestat or sorbinil inhibits tissue AR activity but does not significantly affect plasma lipoprotein levels, or affect the body weight of the mice or their general health. Accumulation of cholesterol-rich foam cells is significantly increased in aortic roots of tolrestat-fed mice[3]. MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. \| \| \| \| \| \| \| \| \| \| [1]. Sestanj K, et al. N-[5-(trifluoromethyl)-6-methoxy-1-naphthalenyl]thioxomethyl]- N-methylglycine (Tolrestat), a potent, orally active aldose reductase inhibitor. J Med Chem. 1984 Mar 27(3):255-6. [Content Brief] [2]. Simard-Duquesne N, et al. The effects of a new aldose reductase inhibitor (tolrestat) in galactosemic and diabetic rats. Metabolism. 1985 Oct 34(10):885-92. [Content Brief] [3]. Srivastava S, et al. Aldose reductase protects against early atherosclerotic lesion formation in apolipoprotein E-null mice. Circ Res. 2009 Oct 9 105(8):793-802. [Content Brief]
Supplier Website	https://www.medchemexpress.com/Tolrestat.html
Last Update	2025-05-21 16:50:25

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