Statil
(Synonyms: 波来瑞斯,ICI 128436,MK-538,Ponalrestat) 目录号 : GC10958
An aldose reductase 2 inhibitor
Cas No.:72702-95-5
Sample solution is provided at 25 µL, 10mM.
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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.
| Cas No. | 72702-95-5 | SDF | |
| 别名 | 波来瑞斯,ICI 128436,MK-538,Ponalrestat | ||
| 化学名 | 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 | ||
| 分子式 | C17H12BrFN2O3 | 分子量 | 391.2 |
| 溶解度 | ≤2mg/ml in ethanol;2mg/ml in DMSO;2mg/ml in dimethyl formamide | 储存条件 | Store at -20°C |
| General tips | 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。 储备液的保存方式和期限：-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 2.5562 mL | 12.7812 mL | 25.5624 mL |
| 5 mM | 0.5112 mL | 2.5562 mL | 5.1125 mL |
| 10 mM | 0.2556 mL | 1.2781 mL | 2.5562 mL |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
3. 以上所有助溶剂都可在 GlpBio 网站选购。
Quality Control & SDS
- View current batch:
- Purity: >99.50%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet