| CAS |
No.222638-67-7 |
| 英文名称 |
BEC Hydrochloride |
| 别名 |
;BECHCl;S-(2-boronoethyl)-L-cysteine.;Aricept，E-2020DonepezilHCl; |
| 分子式 |
C5H12BNO4S·HCl |
| 分子量 |
229.48 |
| 溶解性 |
Soluble in DMSO |
| 纯度 |
≥98% |
| 外观(性状) |
White to off-white Solid |
| 储存条件 |
Powder:-20℃，2 years;Insolvent(母液):-20℃，6 months;-80℃，1 year |
| 运输条件 |
冷藏运输 |
| MDL |
MFCD03453539 |
| SMILES |
B(CCSC[C@@H](C(=O)O)N)(O)O.Cl |
| 靶点 |
Arginase |
| 通路 |
Metabolic Enzyme&Protease |
| 背景说明 |
BEC Hydrochloride是一个竞争性的 Arginase II抑制剂。 |
| 生物活性 |
BEC hydrochloride is a slow-binding and competitive Arginase II inhibitor with Ki of 0.31 μM and 30 nM at pH 7.5 and pH 9.5, respectively[1]. |
| IC50 |
Ki: 0.31μM(BEC hydrochloride，at pH 7.5) and 30nM(BEC hydrochloride，at pH 9.5)[1] |
| In Vitro |
The X-ray crystal structure of the arginase-BEC complex has been determined at 2.3 resolution from crystals perfectly twinned by hemihedry. The structure of the complex reveals that the boronic acid moiety undergoes nucleophilic attack by metal-bridging hydroxide ion to yield a tetrahedral boronate anion that bridges the binuclear manganese cluster，thereby mimicking the tetrahedral intermediate(and its flanking transition states)in the arginine hydrolysis reaction[2]. |
| In Vivo |
Administration of the arginase inhibitor BEC decreases arginase activity and causes alterations in NO homeostasis，which are reflected by increases in S-nitrosylated and nitrated proteins in the lungs from inflamed mice. BEC enhances perivascular and peribronchiolar lung inflammation，mucus metaplasia，NF-κB DNA binding，and mRNA expression of the NF-κB-driven chemokine genes CCL20 and KC，and leads to further increases in airways hyperresponsiveness[3]. |
| 数据来源文献 |
[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. |
| 规格 |
1mg 5mg 10mg 25mg 50mg |
| 单位 |
瓶 |
中文
英语
说明书下载
京公网安备 11011202000391号