Home Neuronal Signaling Histamine Receptor antagonist Azelastine HCl

Azelastine HCl

Catalog No.S2552

For research use only.

Azelastine HCl is a potent, second-generation, selective, histamine receptor antagonist, used in the treatment of rhinitis.

Azelastine HCl Chemical Structure

CAS No. 79307-93-0

Selleck's Azelastine HCl has been cited by 5 Publications

Purity & Quality Control

Choose Selective Histamine Receptor Inhibitors

Related Compound Libraries

Other Histamine Receptor Products

Download Inhibitor Catalog

Download Inhibitor Catalog
Histamine Receptor Signaling Pathways

Histamine Receptor Signaling Pathway Map

Biological Activity

Description Azelastine HCl is a potent, second-generation, selective, histamine receptor antagonist, used in the treatment of rhinitis.
Targets
Histamine receptor [1]
In vitro

Azelastine inhibits Ag- and ionomycin-induced TNF-alpha release with IC50 values of 25.7 mM and 1.66 mM, respectively, in a rat mast RBL-2H3 cell line. Azelastine also inhibits TNF-alpha mRNA expression, TNF-alpha protein synthesis and release, and, possibly related to these effects, Ca2+ influx, in Ag-stimulated cells. Azelastine inhibits TNF-alpha release to a greater extent than mRNA expression/protein synthesis and Ca2+ influx in ionomycin-stimulated cells, suggesting that Azelastine inhibits the release process more potently than transcription or production of TNF-alpha by interfering with a signal other than Ca2+. Azelastine added 1 hour after ionomycin stimulation also immediately blocks subsequent release of TNF-alpha, which has been produced in the cells, without affecting Ca2+ influx. Azelastine inhibits ionomycin-induced, but not Ag-induced, protein kinase C translocation to the membranes. [1] Azelastine hydrochloride (Azeptin) dose-dependently suppresses both DNA and protein synthesis in human gingival fibroblasts (HF) and also suppresses blastogenesis of human peripheral blood lymphocytes (PBL). Azelastine hydrochloride (Azeptin) suppresses both inducible nitric oxide synthase-mRNA level and NO generation in mouse peritoneal macrophages. [2] Azelastine inhibits secretion of IL-6, TNF-alpha and IL-8 as well as NF-kappaB activation and intracellular calcium ion levels in normal human mast cells. [3]

Protocol (from reference)

Solubility (25°C)

In vitro

Chemical Information

Molecular Weight 418.36
Formula

C22H24ClN3O.HCl
CAS No. 79307-93-0
Storage 3 years -20°C powder
2 years -80°C in solvent
Smiles CN1CCCC(CC1)N2C(=O)C3=CC=CC=C3C(=N2)CC4=CC=C(C=C4)Cl.Cl

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

mg/kg g μL

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO % % Tween 80 % ddH2O
%DMSO %

Calculation results:

Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Molarity Calculator

Mass Concentration Volume Molecular Weight

Clinical Trial Information

NCT Number Recruitment Interventions Conditions Sponsor/Collaborators Start Date Phases
NCT00612118 Completed Drug: GSK256066|Drug: azelastine hydrochloride Allergic Rhinitis|Rhinitis Allergic Seasonal GlaxoSmithKline February 2008 Phase 2

(data from https://clinicaltrials.gov, updated on 2022-11-29)

Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

Tel: +1-832-582-8158 Ext:3
If you have any other enquiries, please leave a message.

* Indicates a Required Field

Please enter your name.
Please enter your email. Please enter a valid email address.
Please write something to us.
Tags: buy Azelastine HCl | Azelastine HCl ic50 | Azelastine HCl price | Azelastine HCl cost | Azelastine HCl solubility dmso | Azelastine HCl purchase | Azelastine HCl manufacturer | Azelastine HCl research buy | Azelastine HCl order | Azelastine HCl mouse | Azelastine HCl chemical structure | Azelastine HCl mw | Azelastine HCl molecular weight | Azelastine HCl datasheet | Azelastine HCl supplier | Azelastine HCl in vitro | Azelastine HCl cell line | Azelastine HCl concentration | Azelastine HCl nmr