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Pack Size | Price | Availability | Quantity |
---|---|---|---|
10 mg | Inquiry | Backorder | |
50 mg | Inquiry | Backorder |
Description | This novel compound is an orally bioavailable antagonist of P2X3/P2X2/3 receptors, exhibiting potent activity with a pIC50 of 8 in both human and rat, and a pIC50 of 7.3 specifically for the human P2X2/3 receptor. It demonstrates high brain penetration, evidenced by a brain to plasma ratio of 6, and effectively blocks agonist-evoked intracellular Ca2+ flux and inward currents within the nanomolar range (10 nM to 1 µM) in cell lines that express human P2X3 and P2X2/3 receptors recombinantly. The compound also shows favorable pharmacokinetic properties, with a half-life (t1/2) of 1.63 hours and a time to reach maximum concentration (Tmax) of 30 minutes. |
Alias | P2X3 Purinergic Receptor Antagonist, AF353, P2X2/3 Purinergic Receptor Antagonist, AF353 |
Molecular Weight | 436.68 |
Formula | C14H17IN4O2?HCl |
Cas No. | 927887-18-1 |
Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year |
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