ZM241385

MCE 国际站：ZM241385

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 A_2a 受体 (A_2AR) 拮抗剂，具有 K_i 值为 1.4 nM^[1][2][3]。 IC50 和目标：Ki：1.4 nM (A_2AR)^[2]  

体外：ZM241385（1 μM；24-48 小时；PC12 细胞）处理可逆转 A_2AR 激动剂 CGS21680 显着上调 A_2AR 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.