产品描述: Tolrestat is a potent, orally active aldose reductase inhibitor with IC50 of 35 nM. |
靶点:
IC50: 35 nM (Aldose Reductase);Reductase |
体内研究:
Tolrestat (1.8 mg/kg per day) causes a reversal to normal RBC sorbitol levels diabetic rats. 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. 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 |
参考文献:
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. |
溶解性:
Soluble in DMSO |
保存条件:
2-8℃ |
配置溶液浓度参考:
|
1mg |
5mg |
10mg |
1 mM |
2.798 ml |
13.992 ml |
27.984 ml |
5 mM |
0.56 ml |
2.798 ml |
5.597 ml |
10 mM |
0.28 ml |
1.399 ml |
2.798 ml |
50 mM |
0.056 ml |
0.28 ml |
0.56 ml |
|
注意: |
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