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Catalog Number | orb2283068 |
---|---|
Category | Small Molecules |
Description | AF-353 hydrochloride |
CAS Number | 927887-18-1 |
MW | 436.68 |
SMILES | O(C1=C(C(C)C)C=C(OC)C(I)=C1)C=2C(N)=NC(N)=NC2.Cl |
Formula | C14H17IN4O2?HCl |
Biological Activity | 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. |
Note | For research use only |
Expiration Date | 12 months from date of receipt. |
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