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Ponalrestat

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Chemical Structure| 72702-95-5 同义名 : ICI 128436;Statil;Statyl.;MK538. Brand name: Statil;Ponalrestat, ICI-128436;MK-538
CAS号 : 72702-95-5
货号 : A417818
分子式 : C17H12BrFN2O3
纯度 : 99%+
分子量 : 391.191
MDL号 : MFCD00204117
存储条件：

粉末 Sealed in dry,Store in freezer, under -20°C

液体 -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 60 mg/mL(153.38 mM)，配合低频超声助溶，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 Aldose reductase 2 (ALR2), catalysing reduction of glucose to sorbitol, is strongly associated with pathogenesis of some of the symptoms of diabetes. Statil is an orally active, selective and noncompetitive ALR with Kis of 7.7 nM and 60 nM for ALR2 and ALR1, respectively[1]. In vitro, Statil (1, 10, 100 μM; 6 h) reduced PGF2α production in response to IL-1 in both cultured endometrial cells and endometrial explants[2]. In vivo, Statil (10 or 50 mg/kg; 8 weeks) reduced sorbitol accumulation in rats indicating efficacy of aldose reductase inhibition[3].
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

2.56mL

0.51mL

0.26mL

12.78mL

2.56mL

1.28mL

25.56mL

5.11mL

2.56mL
参考文献

[1]Ward WH, et al. Ponalrestat: a potent and specific inhibitor of aldose reductase. Biochem Pharmacol. 1990 Jan 15;39(2):337-46

[2]Bresson E, et al. The human aldose reductase AKR1B1 qualifies as the primary prostaglandin F synthase in the endometrium. J Clin Endocrinol Metab. 2011 Jan;96(1):210-9

[3]Calcutt NA, et al. Prevention of sensory disorders in diabetic Sprague-Dawley rats by aldose reductase inhibition or treatment with ciliary neurotrophic factor. Diabetologia. 2004 Apr;47(4):718-24