参考详情:ZM241385 | A2A Receptor Antagonist | MCE
CAS:139180-30-6
品牌:MedChemExpress (MCE)
存储条件:Powder: -20°C, 3 years; 4°C, 2 years.In solvent: -80°C, 6 months; -20°C, 1 month.
生物活性:ZM241385 是一种有效、高亲和力和选择性的腺苷 A2a 受体 (A2AR) 拮抗剂,具有 Ki 值为 1.4 nM[1][2][3]。 IC50 和目标:Ki:1.4 nM (A2AR)[2]
体外:ZM241385(1 μM;24-48 小时;PC12 细胞)处理可逆转 A2AR 激动剂 CGS21680 显着上调 A2AR mRNA 和蛋白水平的现象[ 1]。
体内:ZM241385(0.2 μg/小鼠,0.4 μg/小鼠;腹腔注射;每天;持续 11 周;雌性 C57BL/6 WT 小鼠)治疗可减小肿瘤体积,激活 CD8+ T 细胞并降低频率脾脏 MDSC[4]。
热销产品:Stigmasterol | L-Proline | Cyanine5 NHS ester (iodide) | Asundexian | L-Homocysteine | WZB117 | PF-573228 | Isochlorogenic acid A | PF-3644022 | Phthalic acid mono-2-ethylhexyl ester
研究领域:GPCR/G Protein
作用靶点:Adenosine Receptor
Trending products:Recombinant Proteins | Bioactive Screening Libraries | Natural Products | Fluorescent Dye | PROTAC | Isotope-Labeled Compounds | Oligonucleotides
参考文献:
[1]. Linden J, et al. Characterization of human A(2B) adenosine receptors: radioligandbinding, western blotting, and coupling to G(q) in human embryonickidney 293 cells and HMC-1 mast cells. Mol Pharmacol. 1999 Oct;56(4):705-13.
[2]. Poucher SM, et al. The in vitro pharmacology of ZM 241385, a potent, non-xanthine A2a selective adenosinereceptor antagonist. Br J Pharmacol. 1995 Jul;115(6):1096-102.
[3]. Ludwig S, et al. Impact of combination immunochemotherapies on progression of 4NQO-induced murine oral squamous cell carcinoma. Cancer Immunol Immunother. 2019 Jul;68(7):1133-1141.
[4]. Wang Z, et al. Static magnetic field exposure reproduces cellular effects of the Parkinson's disease drugcandidate ZM241385. PLoS One. 2010 Nov 8;5(11):e13883. doi: 10.1371/journal.pone.0013883.