| CAS NO: | 847163-28-4 |
| 包装 | 价格(元) |
| 1mg | 电议 |
| 5mg | 电议 |
| Physical Appearance | A crystalline solid |
| Storage | Store at -20°C |
| M.Wt | 249.3 |
| Cas No. | 847163-28-4 |
| Formula | C15H11N3O |
| Synonyms | CID 664510 |
| Solubility | ≤5mg/ml in DMSO;25mg/ml in dimethyl formamide |
| Chemical Name | 5-(methylamino)-2-(1-naphthalenyl)-4-oxazolecarbonitrile |
| Canonical SMILES | CNC1=C(C#N)N=C(O1)C2=C3C(C=CC=C3)=CC=C2 |
| 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。 |
ML351 is a potent and selective inhibitor of human 15-lipoxygenase-1 with IC50 value of 200 nM [1][2].
Human lipoxygenases (LOX) are nonheme iron-containing enzymes that catalyze the dioxygenation of polyunsaturated fatty acids (e.g., linoleic acid (LA) and arachidonic acid (AA)) to form hydroperoxy fatty acids [1][2]. Human reticulocyte 15-lipoxygenase-1 is an attractive therapeutic target for its role in atherogenesis, diabetes, Alzheimer’s disease, new-born periventricular leukomalacia, breast cancer, and stroke [2].
ML351 is a potent and selective 15-lipoxygenase inhibitor. ML351 exhibited nanomolar potency and excellent selectivity (>250-fold) versus 5-LOX, platelet 12-LOX, 15-LOX-2, ovine COX-1, and human COX-2. In mouse neuronal HT22 cells, ML351 dose-dependently protected against oxidative glutamate toxicity and completely reversed the increase in 12-HETE following glutamate treatment [2][3].
In permanent focal ischemia mice model, IP administration of ML351 resulted in a ~30% reduction in infarct size [2][3].
References:
[1]. Rai G, Joshi N, Perry S, et al. Discovery of ML351, a Potent and Selective Inhibitor of Human 15-Lipoxygenase-1. Probe Reports from the NIH Molecular Libraries Program [Internet]. Bethesda (MD): National Center for Biotechnology Information (US); 2010-2013 Apr 15 [updated 2014 Jan 13].
[2]. Rai G, Joshi N, Jung JE, et al. Potent and selective inhibitors of human reticulocyte 12/15-lipoxygenase as anti-stroke therapies. J Med Chem. 2014 May 22;57(10):4035-48.
[3]. Gaffney BJ. Lipoxygenases: structural principles and spectroscopy. Annu Rev Biophys Biomol Struct. 1996;25:431-59.
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