An active metabolite of azelastine
Related Products
Parent Compound(s)
20873Azelastine (hydrochloride)
Technical Support & Resources

Information provided in the product description is from published literature. Due to the nature of scientific experimentation, your results (e.g., selectivity and effective concentrations) or specific application for this product may differ. If you have questions about how this product fits your application, please contact our technical support staff.

Visit our FAQ

Contact Us

Toll Free Phone (USA and Canada Only): (888) 526-5351
Direct Phone: (734) 975-3888

Request Technical Support

Technical Support Request

To streamline the process attach the appropriate questionnaire to your inquiry.

Download IHC QuestionnaireDownload WB Questionnaire

View Our Privacy Statement for details on how we use and protect your data. In addition, this site is protected by hCaptcha and its Privacy Policy and Terms of Service apply.

N-desmethyl Azelastine

Item No. 35429

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
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(Learn about Variance in 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
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
Recommended Products

Certificates of Analysis & Batch Specific Data

Provide batch numbers separated by commas to download or request available product inserts, QC sheets, certificates of analysis, data packs, and GC-MS data.

Download most recent Certificate of Analysis for this product

    1 mg

    $49

    Add

    5 mg

    $158

    Add

    10 mg

    $218

    Add
    Cayman Chemical
    Neutrophil Biology Wall Poster

    Explore how neutrophils shape the immune response in health and disease. This poster highlights neutrophil pathogen defense mechanisms, including phagocytosis, degranulation, and NETosis, as well as neutrophil roles in inflammation and NET-associated pathologies.

    DOWNLOAD NOW
    Product Description

    N-desmethyl Azelastine is an active metabolite of the histamine H1 receptor antagonist azelastine (Item No. 20873).1,2 It is formed from azelastine primarily by the cytochrome P450 (CYP) isoforms CYP3A4 and CYP2D6 and, to a lesser extent, by CYP1A2.2 N-desmethyl Azelastine (1 µM) inhibits acetylcholine-induced depolarization and contractions in isolated human tracheal smooth muscle.1 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).3

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Richards, I.S., Miller, L., Solomon, D., et al. Azelastine and desmethylazelastine suppress acetylcholine-induced contraction and depolarization in human airway smooth muscle. Eur. J. Pharmacol. 186(2-3), 331-334 (1990).

    2. Nakajima, M., Nakamura, S., Tokudome, S., et al. Azelastine N-demethylation by cytochrome P-450 (CYP)3A4, CYP2D6, and CYP1A2 in human liver microsomes: Evaluation of approach to predict the contribution of multiple CYPs. Drug Metab. Dispos. 27(12), 1381-1391 (1999).

    3. Katoh, M., Nakajima, M., Yamazaki, H., et al. Inhibitory effects of CYP3A4 substrates and their metabolites on P-glycoprotein-mediated transport. Eur. J. Pharm. Sci. 12(4), 505-513 (2001).