BEC HCl

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

BEC HCl 是一种竞争性精氨酸酶抑制剂，结合缓慢。对于精氨酸酶 II，BEC HCl 的 Ki 为 0.31 μM (pH7.5)；对于大鼠精氨酸酶 I，BEC HCl 的 Ki 为 0.4-0.6 μM。

BEC HCl is a competitive arginase inhibitor, which bind slowly. Ki of BEC HCl is 0.31 μM (pH7.5) for Arginase II, and is 0.4-0.6 μM for rat Arginase I.

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.

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).

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GPCR/G Protein

Antibacterial

Arginase-2| rat Arginase I

Cancer

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222638-67-7

229.49

C5H12BNO4S·ClH

>98% (HPLC)

H2O : ≥ 35 mg/mL; 152.51 mM

C(=O)([C@H](CSCCB(O)O)N)O.Cl

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(-20℃)

With Ice Pack

≥ 2 years