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Zopolrestat

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Chemical Structure| 110703-94-1 同义名 : CP73850
CAS号 : 110703-94-1
货号 : A739662
分子式 : C19H12F3N3O3S
纯度 : 99%+
分子量 : 419.377
MDL号 : MFCD00865476
存储条件：

粉末 Sealed in dry,2-8°C

液体 -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 105 mg/mL(250.37 mM)，配合低频超声，并水浴加热至45℃助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO
动物实验配方：
生物活性
描述 Zopolrestat is a potent, orally active aldose reductase (AR) inhibitor with an IC50 of 3.1 nM[1]. Zopolrestat reduced infarct size by up to 61%, both in vitro (2 nM to 1 μM; EC50 = 24 nM) and in vivo (50 mg/kg). Zopolrestat reduced myocardial sorbitol concentration (index of AR activity) by >50%[2]. In the EIU rat eye AqH, both the number of infiltrating cells and protein concentrations of the inflammatory markers, TNF-alpha, NO, and PGE(2) were significantly higher than in the control rats, and inhibition of AR by zopolrestat (25 mg/kg, i.p.) suppressed the LPS-induced increases. The LPS-induced increased expression of AR, TNF-alpha, iNOS, and COX-2 proteins in the ciliary body, corneal epithelium, and retinal wall was also significantly inhibited by zopolrestat[3]. In addition, AR inhibitors (Zopolrestat) negate diabetes-evoked hypertension via ameliorating impaired endothelial relaxation and NO production[4]. Zopolrestat also exerts a protective effect on the slowly developing diabetic cataract, as well as reducing albuminuria and proteinuria[5].
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

2.38mL

0.48mL

0.24mL

11.92mL

2.38mL

1.19mL

23.84mL

4.77mL

2.38mL
参考文献

[1]Mylari BL, Larson ER, Beyer TA, Zembrowski WJ, Aldinger CE, Dee MF, Siegel TW, Singleton DH. Novel, potent aldose reductase inhibitors: 3,4-dihydro-4-oxo-3-[[5-(trifluoromethyl)-2-benzothiazolyl] methyl]-1-phthalazineacetic acid (zopolrestat) and congeners. J Med Chem. 1991 Jan;34(1):108-22.

[2]Tracey WR, Magee WP, Ellery CA, MacAndrew JT, Smith AH, Knight DR, Oates PJ. Aldose reductase inhibition alone or combined with an adenosine A(3) agonist reduces ischemic myocardial injury. Am J Physiol Heart Circ Physiol. 2000 Oct;279(4):H1447-52.

[3]Yadav UC, Srivastava SK, Ramana KV. Aldose reductase inhibition prevents endotoxin-induced uveitis in rats. Invest Ophthalmol Vis Sci. 2007 Oct;48(10):4634-42.

[4]Badawy D, El-Bassossy HM, Fahmy A, Azhar A. Aldose reductase inhibitors zopolrestat and ferulic acid alleviate hypertension associated with diabetes: effect on vascular reactivity. Can J Physiol Pharmacol. 2013 Feb;91(2):101-7.

[5]Beyer-Mears A, Mistry K, Diecke FP, Cruz E. Zopolrestat prevention of proteinuria, albuminuria and cataractogenesis in diabetes mellitus. Pharmacology. 1996 May;52(5):292-302.