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MedChemExpressModel ZM241385 - 139180-30-6

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ZM241385 is a potent, high affinity and selective adenosine A2a receptor (A2AR) antagonist with a Ki value of 1.4 nM[1][2][3].
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ZM241385

MCE China:ZM241385

Brand:MedChemExpress (MCE)

Cat. No.HY-19532

CAS:139180-30-6

Purity:99.45%

Storage:Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year

Shipping:Room temperature in continental US; may vary elsewhere.

Description:ZM241385 is a potent, high affinity and selective adenosine A2a receptor (A2AR) antagonist with a Ki value of 1.4 nM.

In Vitro:ZM241385 (1 μM; 24-48 hours; PC12 cells) treatment reverses the phenomenon that A2AR agonist CGS21680 significantly upregulates A2AR mRNA and protein levels[1].

In Vivo: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].

IC50 & Target:A2AR 1.4 nM (Ki)

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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.  [Content Brief]

[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.  [Content Brief]

[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.  [Content Brief]

[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.  [Content Brief]

Brand introduction:
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