Chemical Structure : VG081821
货号: 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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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.
| 分子量 | 392.42 | |
| 分子式 | C19H20N8O2 | |
| 外观性状 | Solid | |
| 储存条件 |
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| Solubility |
10 mM in DMSO |
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1. Sun S, et al. Drug Dev Res. 2025 Aug;86(5):e70133.
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