Imaradenant (AZD4635, HTL1071) is an oral A2AR antagonist that binds to human A2AR with a Ki of 1.7 nM and with > 30-fold selectivity over other adenosine receptors.
Storage Temp
Store at -20°C
Shipped In
Ice chest + Ice pads
Grade
Moligand™
Action Type
ANTAGONIST
Mechanism of action
Adenosine A2a receptor antagonist
Product Description
Information
Imaradenant (AZD4635) Imaradenant (AZD4635, HTL1071) is an oral A2AR antagonist that binds to human A2AR with a Ki of 1.7 nM and with > 30-fold selectivity over other adenosine receptors.
Targets
A2AR (Cell-free) 1.7 nM(Ki)
In vitro
In CHO cells stably expressing human A2AR, the IC50s of AZD4635 for inhibition of cAMP production are 0.79, 10.0 and 142.9 nM in the presense of 0.1, 1 and 10 μM adenosine, respectively.
In vivo
Blockade of A2AR signaling with AZD4635 could reduce tumor burden and enhance antitumor immunity.
1.Borodovsky A, Barbon CM, Wang Y, Ye M, Prickett L, Chandra D, Shaw J, Deng N, Sachsenmeier K, Clarke JD et al.. (2020) Small molecule AZD4635 inhibitor of A 2A R signaling rescues immune cell function including CD103 + dendritic cells enhancing anti-tumor immunity. J Immunother Cancer, 8 (2):(e000417). [PMID:32727810]
2.A-González N, Castrillo A. (2011) Liver X receptors as regulators of macrophage inflammatory and metabolic pathways.. Biochim Biophys Acta, 1812 (8):(982-94). [PMID:21193033]
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L2313374