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首页-小分子抑制剂&激动剂-GPCR-Adenosine Receptor-VG081821
VG081821

Chemical Structure : VG081821

CAS No.: 2407822-06-2

VG081821 (VG-081821)

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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纯度 & COA & 质检文件 纯度: >98% (HPLC)

生物&药学活性

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.

物理化学性质&存储条件

分子量 392.42
分子式 C19H20N8O2
外观性状 Solid
CAS No.
储存条件
固体粉末
-20°C 12 个月; 4°C 6 个月
配置液
-80°C 6 个月; -20°C 6 个月
Shipping
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

参考文献

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

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