产品
编 号：F279824
分子式：C5H13BClNO4S
分子量：229.49
分子式：C5H13BClNO4S
分子量：229.49
产品类型
规格
价格
是否有货
10mM*1mL in DMSO
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1mg
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5mg
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10mg
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25mg
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50mg
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结构图
CAS No: 222638-67-7
产品详情
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.
体内研究：
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).
体外研究：
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.
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.
体内研究：
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).
体外研究：
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.
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