S80551 |
BEC hydrochloride |
源葉(MedMol) | 98% |
- 提示:詳情請下載說明書。
- 產(chǎn)品描述: 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
- 靶點: Ki: 0.31 μM (BEC hydrochloride, at pH 7.5) and 30 nM (BEC hydrochloride, at pH 9.5);Arginase
- 體外研究:
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.
- 體內(nèi)研究:
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. Animal Model: C57BL/6J wild-type mice, mice deficient in arginase 2 (Arg2-/-), mice deficient in both arginase 1 and 2 (Arg1-/-Arg2-/-), and mice deficient in NOX2 (NOX2-/- Dosage: 20 mg/kg. Administration: I.V., in 0.9% saline, 1 hour before the injection of LPS. Result: BEC robustly reduced VEGF expression in neuroglia (72% reduction) and macrophage/microglia (87% reduction).
- 參考文獻:
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.
- 溶解性: Soluble in DMSO、H2O
- 保存條件: -20℃
- 配置溶液濃度參考:
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:部分產(chǎn)品我司僅能提供部分信息,我司不保證所提供信息的權(quán)威性,僅供客戶參考交流研究之用。
輸入產(chǎn)品批號:
本計算器可幫助您計算出特定溶液中溶質(zhì)的質(zhì)量、溶液濃度和體積之間的關(guān)系,公式為:
質(zhì)量 (mg) = 濃度 (mM) x 體積 (mL) x 分子摩爾量 (g/mol)