| CAS NO: | 72702-95-5 |
| 包装 | 价格(元) |
| 10mg | 电议 |
| 25mg | 电议 |
| 50mg | 电议 |
| Physical Appearance | A crystalline solid |
| Storage | Store at -20°C |
| M.Wt | 391.2 |
| Cas No. | 72702-95-5 |
| Formula | C17H12BrFN2O3 |
| Synonyms | ICI 128436,MK-538,Ponalrestat |
| Solubility | ≤2mg/ml in ethanol;2mg/ml in DMSO;2mg/ml in dimethyl formamide |
| Chemical Name | 3-[(4-bromo-2-fluorophenyl)methyl]-3,4-dihydro-4-oxo-1-phthalazineacetic acid |
| Canonical SMILES | BrC1=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。 |
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.
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