| 产品描述: | 精氨酸酶抑制剂;Arginase Inhibitors;;InformationBEC HCl BEC HCl is a slow-binding, and competitive arginase inhibitor with K i of 0.31 μM (pH7.5) and 0.4-0.6 μM for Arginase II and rat Arginase I, respectively.TargetsArginase II ; rat Arginase I 0.31 μM(Ki); <0.6 μM(Ki)In vitroBEC causes significant enhancement of NO-dependent smooth muscle relaxation. In myocytes, BEC augments Ca(2+)-dependent NOS activity and NO production, and increases basal contractility. BEC also inhibits the proliferation of human pulmonary artery smooth muscle cells by decreasing the expression levels of cyclin D1 and CDK4, increasing the expression of p27, and partly reducing the phosphorylation of Akt and ERK.In vivoIn mice with allergic inflammation (OVA/OVA), BEC enhances peribronchiolar and perivascular inflammation, leads to enhanced NF-κB DNA binding and NF-κB-dependent inflammatory gene expression, and causes an increase in the content of NOx. In rats with pulmonary arterial hypertension, BEC reduces the right ventricle systolic pressure. |
| 靶点: |
Ki: 0.31 μM (BEC hydrochloride, at pH 7.5) and 30 nM (BEC hydrochloride, at pH 9.5) |
| 体内研究: |
服用精氨酸酶抑制剂 BEC 可降低精氨酸酶活性并导致 NO 稳态改变,这反映在炎症小鼠肺中 S-亚硝基化和硝化蛋白的增加。BEC 增强血管周围和细支气管周围肺部炎症、黏液化生、NF-κB DNA 结合以及 NF-κB 驱动的趋化因子基因 CCL20 和 KC 的 mRNA 表达,并导致气道高反应性进一步增强。 |
| 参考文献: |
1. Colleluori DM, et al. Classical and slow-binding inhibitors of human type II arginase. Biochemistry. 2001 Aug 7;40(31):9356-62. 2. Kim NN, et al. Probing erectile function: S-(2-boronoethyl)-L-cysteine binds to arginase as a transition state analogue and enhances smooth muscle relaxation in human penile corpus cavernosum. Biochemistry. 2001 Mar 6;40(9):2678-88. 3. Ckless K, et al. Inhibition of arginase activity enhances inflammation in mice with allergic airway disease, in association with increases in protein S-nitrosylation and tyrosine nitration. J Immunol. 2008 Sep 15;181(6):4255-64. |
| 保存条件: |
-80℃(运输条件:冰袋低温运输) |
| 配置溶液浓度参考: |
|
1mg |
5mg |
10mg |
| 1 mM |
4.357 ml |
21.787 ml |
43.575 ml |
| 5 mM |
0.871 ml |
4.357 ml |
8.715 ml |
| 10 mM |
0.436 ml |
2.179 ml |
4.357 ml |
| 50 mM |
0.087 ml |
0.436 ml |
0.871 ml |
|
| 注意: |
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