PQ 69

PQ 69 是一种有效的选择性腺苷 A1 受体拮抗剂，具有反向激动剂活性。

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10mg

￥4887.00

3910.00

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50mg

￥20387.00

16310.00

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Background

Potent and selective A1 receptor inverse agonist. Exhibits high binding affinity at A1 receptor (Ki values are 0.07 and 0.96 nM for rat and human receptors respectively). Reduces basal [35S]-GTPγS binding 44.6% (IC50 = 0.19 nM). Antagonizes the effects of A1 agonist R-PIA (IC50 = 18.3 nM) and exhibits competitive antagonism on CCPA-induced tracheal contractions ex vivo. Displays 217- fold selectively over hA2A receptor and >1000-fold selectivity over hA3 receptor.

Lu et al (2014) PQ-69, a novel and selective adenosine A1 receptor antagonist with inverse agonist activity. Purinergic Signal. 10 619 PMID:25248972