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VG081821

Chemical Structure : VG081821

CAS No.: 2407822-06-2

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VG081821 (VG-081821)

Catalog No.: PC-25168Not For Human Use, Lab Use Only.

VG081821 is a potent, selective, orally active A2A adenosine receptor antagonist with binding Ki of 0.85 nM, >300-fold selective over A1, A2B, and A3 receptors.

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Purity & Documentation Purity: >98% (HPLC)

Biological Activity

VG081821 is a potent, selective, orally active A2A adenosine receptor antagonist with binding Ki of 0.85 nM, >300-fold selective over A1, A2B, and A3 receptors.
VG081821 down-regulates intracellular cAMP levels by the cAMP TR-FRET assay with IC50 of 5.77 nM.
VG081821 is simultaneously a highly potent antagonist and inverse agonist of A2A receptor, has the inverse agonistic EC50 values of 0.74 nM.
VG081821 exhibits lower intrinsic clearance and superior pharmacokinetic profile compared to ZM241385.

Physicochemical Properties

M.Wt 392.42
Formula C19H20N8O2
Appearance Solid
CAS No.
Storage
Solide Powder
-20°C 12 Months; 4°C 6 Months
In Solvent
-80°C 6 Months; -20°C 6 Months
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Solubility

10 mM in DMSO
Chemical Name/SMILES

2-(furan-2-yl)-N5-(4-(oxetan-3-ylamino)phenethyl)-[1,2,4]triazolo[1,5-a][1,3,5]triazine-5,7-diamine

References

1. Sun S, et al. Drug Dev Res. 2025 Aug;86(5):e70133.

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