8pyDTZ is a pyridyl diphenylterazine (DTZ) analog designed for bioluminescent imaging, specifically optimized for use with the LumiLuc luciferase system. In the presence of pyridyl substrates 8pyDTZ, LumiLuc generates highly bright yellow bioluminescence. 8pyDTZ offers enhanced water solubility and red-shifted emission, making it suitable for in vivo imaging applications[1]. 8pyDTZ has about 13 times better aqueous solubility and bioavailability than DTZ. The emission from 8-pyDTZ/LumiLuc was about 5 times brighter than 8-pyDTZ/teLuc[2].
In vitro, the 8pyDTZ (30µM) can been used to quantify biomarkers such as human serum albumin (HSA) in serum samples and α-amylase in saliva samples by incubating the analyte of interest for 30min at 25℃[3].
In vivo, 8pyDTZ (0.2μmol/mouse) in 100μL normal saline is administrated into luciferase expressing HeLa cells xenograft mouse model via intravenous delivery to track tumor growth with high sensitivity and good tissue penetration ability[1].
References:
[1] Yeh H W, Xiong Y, Wu T C, et al. ATP-Independent Bioluminescent Reporter Variants To Improve in Vivo Imaging. ACS Chem Biol. 2019 May 17;14(5):959-965.
[2] Syed A J, Anderson J C. Applications of bioluminescence in biotechnology and beyond. Chem Soc Rev. 2021 May 7;50(9):5668-5705.
[3] Guo Z, Parakra R D, Xiong Y, et al. Engineering and exploiting synthetic allostery of NanoLuc luciferase. Nat Commun. 2022 Feb 10;13(1):789.
8pyDTZ是一种吡啶基二苯基特拉嗪（DTZ）类似物，专为生物发光成像而设计，特别针对LumiLuc荧光素酶系统进行了优化。在吡啶基底物8pyDTZ的存在下，LumiLuc产生高度明亮的黄色生物发光。8pyDTZ提供增强的水溶性和红移发射，使其适合体内成像应用[1]。8pyDTZ的水溶性和生物利用度是DTZ的13倍。8-pyDTZ/LumiLuc的辐射亮度约为8-pyDTZ/teLuc的5倍[2]。
在体外，8pyDTZ（30µM）可用于定量血清样品中的人血清白蛋白（HSA）和唾液样品中的α-淀粉酶等生物标志物，在25℃下孵育30min[3]。
在体内，将100μL生理盐水中的8pyDTZ （0.2μmol/只）静脉给药到表达荧光素酶的HeLa细胞异种移植小鼠模型中，以高灵敏度和良好的组织穿透能力跟踪肿瘤生长[1]。