Biological Activity
Potent and selective A1 receptor antagonist/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.
Technical Data
M. Wt | 350.39 |
Formula | C20H19FN4O |
Storage | Store at +4°C |
Purity | ≥98% (HPLC) |
CAS Number | 910045-32-8 |
PubChem ID | 121513859 |
InChI Key | FJRYQRBEISYVBB-UHFFFAOYSA-N |
Smiles | O=C1N(C4=CC(F)=CC=C4)NC2=C1C(NCCCC)=NC3=C2C=CC=C3 |
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
All Tocris products are intended for laboratory research use only.
Solubility Data
Solvent | Max Conc. mg/mL | Max Conc. mM | |
---|---|---|---|
Solubility | |||
DMSO | 35.04 | 100 | |
ethanol | 3.5 | 10mM with gentle warming |
Preparing Stock Solutions
The following data is based on the product molecular weight 350.39. Batch specific molecular weights may vary from batch to batch due to solvent of hydration, which will affect the solvent volumes required to prepare stock solutions.
Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
---|---|---|---|
1 mM | 2.85 mL | 14.27 mL | 28.54 mL |
5 mM | 0.57 mL | 2.85 mL | 5.71 mL |
10 mM | 0.29 mL | 1.43 mL | 2.85 mL |
50 mM | 0.06 mL | 0.29 mL | 0.57 mL |
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References
References are publications that support the products' biological activity.
Lu et al (2014) PQ-69, a novel and selective adenosine A1 receptor antagonist with inverse agonist activity. Purinergic Signal. 10 619 PMID: 25248972
Keywords: PQ 69, supplier, PQ69, Potent, selective, A1, antagonists, receptors, adenosines, inverse, agonists, Adenosine, A1, Receptors, Adenosine, A1, Receptors, Tocris Bioscience