BEC HCl

製品コードS7929 バッチS792901

印刷

化学情報

Chemical Structure Synonyms N/A Storage
(From the date of receipt)		 3 years -20°C powder
1 years -80°C in solvent
化学式

C5H12BNO4S.HCl
分子量 229.49 CAS No. 222638-67-7
Solubility (25°C)* 体外 DMSO 45 mg/mL (196.08 mM)
Water 45 mg/mL (196.08 mM)
Ethanol 45 mg/mL (196.08 mM)
体内 （毎回新しく調製した物を用意してください）
Homogeneous suspension
CMC-NA
≥5mg/ml Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Clear solution
5%DMSO 40%PEG300 5%Tween80 50%ddH2O

この製剤はselleckのラボで検証済みです。上記の溶解方法がご要望を満たさない場合、selleckの営業担当までお問い合わせ頂ければ、個別の試験を行います。

 2.250mg/ml (9.80mM) Taking the 1 mL working solution as an example, add 50 μL of 45 mg/ml clarified DMSO stock solution to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to clarify; then continue to add 500 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results. 
Clear solution
5% DMSO 95% Corn oil

この製剤はselleckのラボで検証済みです。上記の溶解方法がご要望を満たさない場合、selleckの営業担当までお問い合わせ頂ければ、個別の試験を行います。

 0.560mg/ml (2.44mM) Taking the 1 mL working solution as an example, add 50 μL of 11.2 mg/ml clear DMSO stock solution to 950 μL of corn oil and mix evenly. The mixed solution should be used immediately for optimal results. 
* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

溶剤液（一定の濃度）を調合する

生物活性

製品説明 BEC HCl is a slow-binding, and competitive arginase inhibitor with Ki of 0.31 μM (pH7.5) and 0.4-0.6 μM for Arginase II and rat Arginase I, respectively.
in vitro BEC causes significant enhancement of NO-dependent smooth muscle relaxation. [2] In myocytes, BEC augments Ca(2+)-dependent NOS activity and NO production, and increases basal contractility. [3] 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. [5]
in vivo In 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. [4] In rats with pulmonary arterial hypertension, BEC reduces the right ventricle systolic pressure. [5]

プロトコル(参考用のみ)

キナーゼアッセイ Enzyme Assays
Assays of hAII activity utilizing agmatine as a substrate are performed at pH 7.5 with [guanido-14C]agmatine replacing l-[guanido-14C]arginine in the assay and with increasing concentrations of unlabeled agmatine. Evaluation of inhibitors is performed using the radioactive arginase assay containing 100 μM MnCl2 and either 100 mM HEPES−KOH, pH 7.5, or 100 mM CHES−KOH, pH 9.5. NOHA and nor-NOHA are evaluated as inhibitors of hAII at pH 7.5 by the addition of 2, 4, 6, and 10 μM NOHA or 0.05, 0.1, 0.2, and 0.3 μM nor-NOHA to the assay mixture. ABH and BEC are similarly evaluated as inhibitors of hAII at pH 7.5 by the addition of 0.1, 0.5, 1, and 2 μM ABH and 0.5, 1, 2, and 4 μM BEC to the assay mixture. Inhibition data are fit to the equation for competitive inhibition using the programs of Cleland. Inhibition constants for NOHA at pH 9.5 and for weak classical inhibitors (Ki > 5 mM) at pH 7.5 are determined by titrating a standard assay mixture containing 5 mM arginine with increasing concentrations of inhibitor. The Ki is estimated from the equation for competitive inhibition, although complete inhibition patterns are not determined for weak hAII inhibitors. Enzyme activity with l-argininamide, l-canavanine, l-homoarginine, and l-argininic acid as alternate substrates is measured with a coupled, spectrophotometric assay with urease and glutamate dehydrogenase.
動物実験 動物モデル Mice with allergic inflammation (OVA/OVA)
投薬量 0.30 mM, 40 μl
投与方法 oropharyngeal aspiration

参考

  • https://pubmed.ncbi.nlm.nih.gov/11478904/
  • https://pubmed.ncbi.nlm.nih.gov/11258879/
  • https://pubmed.ncbi.nlm.nih.gov/16537391/
  • https://pubmed.ncbi.nlm.nih.gov/18768883/
  • https://pubmed.ncbi.nlm.nih.gov/26126810/

Selleckの高級品が、幾つかの出版された研究調査結果（以下を含む）で使われた：

Sugar and arginine facilitate oral tolerance by ensuring the functionality of tolerogenic immune cell subsets in the intestine [ Cell Rep, 2024, 43(7):114490] PubMed: 38990720
l-arginine promotes angio-osteogenesis to enhance oxidative stress-inhibited bone formation by ameliorating mitophagy [ J Orthop Translat, 2024, 46:53-64] PubMed: 38808262
Warburg effect-related risk scoring model to assess clinical significance and immunity characteristics of glioblastoma [ Cancer Med, 2023, 10.1002/cam4.6627] PubMed: 37864422
The KRAS-G12D mutation induces metabolic vulnerability in B-cell acute lymphoblastic leukemia [ iScience, 2022, 25(3):103881] PubMed: 35243242

長期の保管のために-20°Cの下で製品を保ってください。

人間や獣医の診断であるか治療的な使用のためにでない。

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