Hypoxyprobe (Pimonidazole Hydrochloride) 缺氧探針

基本描述：

Hypoxyprobe-1 是2-硝基咪唑的替代物(wù)，其化學名和唯一(yī)成分是Pimonidazole hydrochloride（Pimonidazole HCl），分子量為(wèi)290.8，水(shuǐ)溶性為(wèi)400mM（=116 mg/ml），紫外吸收（324nm）的吸光(guāng)系數為(wèi)7020（0.9%生(shēng)理鹽水(shuǐ)）。

Hypoxyprobe-1的粉末和溶液形式皆具化學穩定性。比如，固體形式的Hypoxyprobe-1于柔弱光(guāng)線下(xià)室溫保存2年(nián)，UV和HPLC分析法評估無任何降解發生(shēng)。溶于0.9%生(shēng)理鹽水(shuǐ)的Hypoxyprobe-1，濃度100g/L置于2-8℃保存4.5年(nián)，UV和HPLC分析法評估無任何降解發生(shēng)。

作用機(jī)制：

缺氧細胞中Pimonidazole被還(hái)原後得以活化。這一(yī)活化的中間物(wù)與蛋白(bái)質、多(duō)肽和氨基酸中的巯基基團（thiol groups）形成穩定的加合物(wù)。Mab1抗體結合這些加合物(wù)從(cóng)而能(néng)借由免疫化學法來檢測。

問：Pimonidazole缺氧探針的活化以及結合到(dào)缺氧細胞上(shàng)的作用機(jī)理如何？

答：Varghese et al. showed that hypoxic cells bind 2-nitroimidazoles to peptide thiols such as glutathione. The current view of the metabolism of pimonidazole is summarized in the scheme below. O2 competes for the addition of the first electron to pimonidazole which accounts for the pO2 dependence of activation and binding. On the basis of test tube experiments, it is estimated that ca 20 % of activated pimonidazole binds to cellular thiols and ca 80% does not bind but is fragmented by reaction with water. Pimonidazole is subject to oxidative metabolism leading to easily excretable N-oxide, sulfate and glucuronate derivatives (ST = sulfotransferase; GT = glucuronly transferase). These oxidative pathways do not appear to interfere with the utility of pimonidazole as a hypoxia marker. 

訂購信息：原裝正品，歡迎來電(diàn)咨詢，電(diàn)話：021-54736159 ，18121428569；QQ：3308240863， 2971634497。

文件(jiàn)下(xià)載：

1. Hypoxyprobe frequently asked questions (FAQ) 常見(jiàn)問題

2. Hypoxyprobe Kit Application 應用文獻

    

    

    — —Written/Edited by V. Shallan【版權歸MKBio懋康所有】

    

    

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