您好,欢迎来到化工原料网! [登录] [免费注册]
化工原料网
位置:首页 > 产品库 > Statil
立即咨询
咨询类型:
     
*姓名:
*电话:
*单位:
Email:
*留言内容:
请详细说明您的需求。
*验证码:
 
Statil
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
Statil图片
CAS NO:72702-95-5
包装与价格:
包装价格(元)
10mg电议
25mg电议
50mg电议

产品介绍

化学性质

Physical AppearanceA crystalline solid
StorageStore at -20°C
M.Wt391.2
Cas No.72702-95-5
FormulaC17H12BrFN2O3
SynonymsICI 128436,MK-538,Ponalrestat
Solubility≤2mg/ml in ethanol;2mg/ml in DMSO;2mg/ml in dimethyl formamide
Chemical Name3-[(4-bromo-2-fluorophenyl)methyl]-3,4-dihydro-4-oxo-1-phthalazineacetic acid
Canonical SMILESBrC1=CC=C(CN2C(C(C=CC=C3)=C3C(CC(O)=O)=N2)=O)C(F)=C1
运输条件蓝冰运输或根据您的需求运输。
一般建议为了使其更好的溶解,请用37℃加热试管并在超声波水浴中震动片刻。不同厂家不同批次产品溶解度各有差异,仅做参考。若实验所需浓度过大至产品溶解极限,请添加助溶剂助溶或自行调整浓度。溶液形式一般不宜长期储存,请尽快用完。

资料参考

IC50: 21.0 nM

Statil, also known as ICI 128436, is an aldose reductase inhibitor, inhibits the conversion of glucose to sorbitol. Statil has the ability to activate the activity of lipoprotein lipase (LPL) both in vivo and in vitro. Also, statil alleviates the cachectic symptoms induced by B16 melanoma in mice. LPL, as a key regulatory enzyme, is responsible for the hydrolysis of triglyceride-rich lipoproteins.

In vitro: Statil strongly, dose-dependently, inhibited the enzyme activity of tumor marker Aldo-keto reductase 1B10. In addition, statil suppressed the cell growth and proliferation dose-dependently in both lung cancer cells NCI-H460 and breast cancer cells BT-20. Also, it was shown that statil induced apoptotic cell death [1].

In vivo: Statil was given to diabetic male rats at 25mg/kg orally by gavage once daily. After five days, statil inhibited rat, bovine, and human aldose reductase and reduced sorbitol levels in sciatic nerve, retina, lens, and renal cortex. Moreover, statil played an important role in rodent models of the lenticular and neural complications of diabetes. And the development of cataracts was completely prevented in diabetic rats at doses as low as 25 mg/kg daily [2].

References:
[1].  Cao, Z., Zhou, B., Chen, X., Huang, D., Zhang, X., & Wang, Z. et al. Statil suppresses cancer cell growth and proliferation by the inhibition of tumor marker AKR1B10. Anti-Cancer Drugs, 2014; 25(8): 930-937.
[2].  Stribling, D., Mirrlees, D., Harrison, H., & Earl, D. Properties of ICI 128,436, a novel aldose reductase inhibitor, and its effects on diabetic complications in the rat. Metabolism, 1985; 34(4): 336-344.