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首页-小分子抑制剂&激动剂-GPCR-Adrenergic Receptor-AP-7-168
AP-7-168

Chemical Structure : AP-7-168

CAS No.: 2816062-15-2

AP-7-168

货号: PC-27918Not For Human Use, Lab Use Only.

AP-7-168 is a specific β-arrestin-biased negative allosteric modulator (NAM) of β2-adrenergic receptor (β2AR), mediates β2AR dimerization with pEC50 of 5.93 in HEK cells, is >1,000-fold effective at inhibiting β-arrestin2 recruitment versus cAMP production.

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纯度 & COA & 质检文件 纯度: >98% (HPLC) Select Batch:

生物&药学活性

AP-7-168 is a specific β-arrestin-biased negative allosteric modulator (NAM) of β2-adrenergic receptor (β2AR), mediates β2AR dimerization with pEC50 of 5.93 in HEK cells, is >1,000-fold effective at inhibiting β-arrestin2 recruitment versus cAMP production.
AP-7-168 shows direct binding to the monomeric β2AR receptor with Kd of 30 uM.
AP-7-168 promotes β2AR dimerization in continuous membranes and in cells.
AP-7-168 (10 uM) caused a slight reduction in the monomer–Gs binding affinity (KD = 1.7 μM) in BLI assays.
AP-7-168 biases TM6 conformational dynamics of β2AR in both dimer and monomer.
AP-7-168-bound β AR dimers inhibits GRK5-mediated phosphorylation of β2AR in both detergent and nanodiscs.

物理化学性质&存储条件

分子量 433.30
分子式 C20H19BrF2N4
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

6-Bromo-N4-cyclohexyl-N2-(3,4-difluorophenyl)-2,4-quinazolinediamine

参考文献

1. Shen J, et al. Nature. 2026 Aug 19. doi: 10.1038/s41586-026-10892-y.

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