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82964-04-3

82964-04-3 structure
82964-04-3 structure

Name tolrestat
Synonyms [(6-Methoxy-5-trifluoromethyl-naphthalene-1-carbothioyl)-methyl-amino]-acetic acid
2-[[6-methoxy-5-(trifluoromethyl)naphthalene-1-carbothioyl]-methylamino]acetic acid
N-{[6-Methoxy-5-(trifluoromethyl)-1-naphthyl]carbothioyl}-N-methylglycine
N-{[6-Methoxy-5-(trifluoromethyl)-1-naphthyl]carbonothioyl}-N-methylglycine
N-[[6-Methoxy-5-(trifluoromethyl)-1-naphthalenyl]thioxomethyl]-N-methylglycine
AY-27,773
Tolrestatum [Latin]
N-(6-Methoxythio-5-(trifluoromethyl)-1-naphthoyl)sarcosine
Alredase
N-{[6-methoxy-5-(trifluoromethyl)naphthalen-1-yl]carbothioyl}-N-methylglycine
Tolrestatum
Tolrestat
Glycine, N-[[6-methoxy-5-(trifluoromethyl)-1-naphthalenyl]thioxomethyl]-N-methyl-
Description Tolrestat is a potent, orally active aldose reductase inhibitor with IC50 of 35 nM.
Related Catalog
Target

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].
Animal Admin 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.
References

[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.

[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.

[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.

Density 1.4±0.1 g/cm3
Boiling Point 498.1±55.0 °C at 760 mmHg
Melting Point 164-165°
Molecular Formula C16H14F3NO3S
Molecular Weight 357.348
Flash Point 255.0±31.5 °C
Exact Mass 357.064636
PSA 81.86000
LogP 3.41
Vapour Pressure 0.0±1.3 mmHg at 25°C
Index of Refraction 1.602
Storage condition 2-8℃