2. Metabolic Enzyme/Protease
  3. Drug Metabolite
  4. Desmethylazelastine

Desmethylazelastine is a main active metabolite of Azelastine that is oxidatively metabolized by the cytochrome P450 enzyme system with a protein binding rate of 97% and an elimination half-life of 54 hours. Azelastine is an orally active, selective and high-affinity histamine H1-receptor antagonist. Azelastine can be used in studies of allergic rhinitis, asthma, diabetic hyperlipidemic and SARS-CoV-2.

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Desmethylazelastine Chemical Structure

Desmethylazelastine Chemical Structure

CAS No. : 47491-38-3

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Desmethylazelastine Related Antibodies

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Description

Desmethylazelastine is a main active metabolite of Azelastine that is oxidatively metabolized by the cytochrome P450 enzyme system with a protein binding rate of 97% and an elimination half-life of 54 hours. Azelastine is an orally active, selective and high-affinity histamine H1-receptor antagonist. Azelastine can be used in studies of allergic rhinitis, asthma, diabetic hyperlipidemic and SARS-CoV-2[1][2][3][4][5].

In Vivo

1.19 Pharmacokinetic parameters of desmethylazelastine after a single oral administration of 1.0 mg/kg azelastine hydrochloride in guinea pigs[1].

Blood Lung
Cmax (ng/mL)[a] 17.6 2863
Tmax (h) 3.0-6.0 4.0-6.0
Tlag (h) 0.25 0.39
AUC0-24 (ng•h/mL)[a] 180 28502
t1/2 (h) 4.24 3.90
CL (L/h) 0.213
Lung-blood ratio[b] 146 146
[a] For lung, the unit in grams (g) instead of milliliter (mL). [b] Mean value calculated from all time points.

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Molecular Weight

367.87

Formula

C21H22ClN3O
CAS No.
SMILES

O=C1C2=C(C(CC3=CC=C(C=C3)Cl)=NN1C4CCNCCC4)C=CC=C2
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Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
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Desmethylazelastine Related Classifications

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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

Desmethylazelastine47491-38-3Drug MetaboliteazelastinemetaboliteSARS-CoV-2asthmaallergic rhinitisdiabetic hyperlipidemicInhibitorinhibitorinhibit

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