N-desmethyl Azelastine

N-desmethyl Azelastine is an active metabolite of the histamine H1 receptor antagonist azelastine (Cay-20873). It is formed from azelastine primarily by the cytochrome P450 (CYP) isoforms CYP3A4 and CYP2D6 and, to a lesser extent, by CYP1A2. N-desmethyl Azelastine (1 µM) inhibits acetylcholine-induced depolarization and contractions in isolated human tracheal smooth muscle. It also inhibits transport of daunorubicin (Cay-14159) and digoxin (Cay-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).Formal Name: 4-[(4-chlorophenyl)methyl]-2-(hexahydro-1H-azepin-4-yl)-1(2H)-phthalazinone. CAS Number: 47491-38-3. Synonyms: DAZ, Desmethylazelastine. Molecular Formula: C21H22ClN3O. Formula Weight: 367.9. Purity: >98%. Formulation: (Request formulation change), A solid. Solubility: DMSO: soluble. SMILES: O=C1C2=CC=CC=C2C(CC3=CC=C(Cl)C=C3)=NN1C4CCNCCC4. InChi Code: InChI=1S/C21H22ClN3O/c22-16-9-7-15(8-10-16)14-20-18-5-1-2-6-19(18)21(26)25(24-20)17-4-3-12-23-13-11-17/h1-2,5-10,17,23H,3-4,11-14H2. InChi Key: WRYCMIFVXDQIKN-UHFFFAOYSA-N.