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Product Description
– A2AR-antagonist-1 (compound 38) is an orally active adenosine A2A receptor (A2AR) antagonist (IC50=29 nM). A2AR-antagonist-1 exhibits anti-tumor activity and mouse liver microsomal metabolic stability (t1/2=86.1 min). A2AR-antagonist-1 is also a T cells activator, via inhibiting immunosuppressive molecules (LAG-3 and TIM-3) and enhancing effector molecules (GZMB, IFNG, and IL-2)[1].
Web ID
– HY-149916
Shipping
– Room temperature
Applications
– Cancer-programmed cell death
Molecular Formula
– C27H25N5O2
References
– [1]Zhu C, et al. Discovery of Pyridinone Derivatives as Potent, Selective, and Orally Bioavailable Adenosine A2A Receptor Antagonists for Cancer Immunotherapy. J Med Chem. 2023 Mar 23.
CAS Number
– 2922920-71-4
Molecular Weight
– 451.52
SMILES
– O=C(N(CC1=CC=CC(C(O)(C)C)=C1)C=C2)C=C2C3=NC(N)=NC(C4=C(C)C(C#N)=CC=C4)=C3
Clinical Information
– No Development Reported
Research Area
– Cancer
Solubility
– 10 mM in DMSO
Target
– Adenosine Receptor
Isoform
– Adenosine A2A receptor (A2AR)
Pathway
– GPCR/G Protein
Product type
– Reference compound
Disclaimer: All products are for Research use only unless clearly stated otherwise on the product datasheet. Datasheets provided on the website are drafts for reference purpose only and you are requested to always refer to the hard copy included in the kit for your experimentation. Agdia Products are available for delivery only in Canada.
