ZM 241385 |
Catalog No.GC11017 |
ZM 241385는 1.4 nM의 Ki 값을 갖는 강력하고 높은 친화도의 선택적 아데노신 A2a 수용체(A2AR) 길항제입니다.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 139180-30-6
Sample solution is provided at 25 µL, 10mM.
ZM241385 is a potent, high affinity and selective adenosine A2a receptor (A2AR) antagonist with a Ki value of 1.4 nM[1][2][3].
ZM241385 (1 μM; 24 hours; PC12 cells) treatment reverses the phenomenon that A2AR agonist CGS21680 significantly upregulates A2AR mRNA levels[1].ZM241385 (1 μM; 48 hours; PC12 cells) treatment reverses the phenomenon that A2AR agonist CGS21680 significantly increases A2AR protein levels[1].
ZM241385 (0.2 μg/mouse, 0.4 μg/mouse; intraperitoneal injection; every day; for 11 weeks; female C57BL/6 WT mice) treatment decreases tumor volume, activates CD8+ T cells and reduces the frequency of splenic MDSC[4].
References:
[1]. 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.
[2]. 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.
[3]. 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.
[4]. 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.
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