Formulation: A solid
Formal Name: 4-[(4-chlorophenyl)methyl]-2-(hexahydro-1H-azepin-4-yl)-1(2H)-phthalazinone
Purity: ≥98%
Formula Markup: C21H22ClN3O
Formula Weight: 367,9
Shelf life (days): 1460
CAS Number: 47491-38-3
Notes: N-desmethyl Azelastine is an active metabolite of the histamine H1 receptor antagonist azelastine (Item No. 20873).{62780,62781} It is formed from azelastine primarily by the cytochrome P450 (CYP) isoforms CYP3A4 and CYP2D6 and, to a lesser extent, by CYP1A2.{62781} N-desmethyl Azelastine (1 µM) inhibits acetylcholine-induced depolarization and contractions in isolated human tracheal smooth muscle.{62780} It also inhibits transport of daunorubicin (Item No. 14159) and digoxin (Item No. 22266) in LLC-GA5-CoL150 cells overexpressing P-glycoprotein (P-gp), also known as multidrug resistance protein 1 (MDR1; IC50s = 11.8 and 41.8 µM, respectively).{62782}