Formulation: A crystalline solid
Formal Name: 5-[5-iodo-4-methoxy-2-(1-methylethyl)phenoxy]-2,4-pyrimidinediamine, monohydrochloride
Purity: ≥98%
Formula Markup: C14H17IN4O2 • HCl
Formula Weight: 436,7
Shelf life (days): 1460
CAS Number: 927887-18-1
Notes: AF-353 is a noncompetitive dual antagonist of the purinoreceptors P2X3 and P2X2/3 (IC50s = 10 and 79.4 nM, respectively).{47203,47204} It is selective for P2X3 and P2X2/3 over P2X1, P2X2, P2X4, P2X5, and P2X7 (IC50 = >10 µM for all).{47204} It inhibits calcium flux in CHO-K1 cells expressing the rat P2X3 receptor and in 1321N1 cells expressing the human P2X3 and P2X2/3 receptors (IC50s = 8.91, 8.71, and 38.9 nM, respectively). AF-353 decreases the electrical signals in the detrusor, but not striated, muscle of the bladder in female rats.{47205}