Choose Your Country or Region

Azelastine HCl

Name: Azelastine HCl
Brand: Selleck Chemicals
SKU: S2552
Rating: 5 (4 reviews)

Catalog No.S2552

For research use only.

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

CAS No. 79307-93-0

Selleck's Azelastine HCl has been cited by 4 Publications

Purity & Quality Control

Choose Selective Histamine Receptor Inhibitors

Related Compound Libraries

Other Histamine Receptor Products

AZD3839^New

AZD3839 is a potent and selective BACE1 inhibitor with K_i of 26.1 nM, about 14-fold selectivity over BACE2. Phase 1.
Xanthohumol^New

Xanthohumol, a prenylated chalcone from hop, inhibits COX-1 and COX-2 activity and shows chemopreventive effects. Xanthohumol inhibits diacylglycerol acyltransferase 1 (DGAT1) and DGAT2 with both IC50 of 40 μM. Xanthohumol is also a potent antiviral agent against a series of DNA and RNA viruses. Xanthohumol induces growth inhibition and apoptosis in cancer cells. Phase 1.
Nirogacestat (PF-03084014)^New

Nirogacestat (PF-03084014, PF-3084014) is a selective gamma-secretase inhibitor with IC50 of 6.2 nM in a cell-free assay. Nirogacestat (PF-03084014, PF-3084014) induces apoptosis. Phase 2.
Loratadine (SCH29851)

Loratadine (SCH29851) is a histamine H1 receptor antagonist, used to treat allergies. Also acts as a selective inhibitor of B(0)AT2 with IC50 of 4 μM.
JNJ-7777120

JNJ-7777120 is the first potent and selective non-imidazole histamine H4 receptor antagonist with K_i of 4.5 nM, exhibits >1000-fold selectivity over the other histamin receptors.
Clemastine (HS-592) fumarate

Clemastine Fumarate (HS-592, Meclastine) is a selective histamine H1 receptor antagonist with IC50 of 3 nM. Clemastine stimulates autophagy via mTOR pathway.
Histamine Phosphate

Histamine acts directly on the blood vessels to dilate arteries and capillaries mediated by both H 1- and H 2-receptors.
Lidocaine

Lidocaine (Alphacaine) is a selective inverse peripheral histamine H1-receptor agonist with an IC50 of >32 μM.
Pemirolast potassium

Pemirolast potassium (BMY26517) is a histamine H1 antagonist and mast cell stabilizer that acts as an antiallergic agent.
Nizatidine

Nizatidine is a histamine H2 receptor antagonist with IC50 of 0.9 nM, also inhibits AChE with IC50 of 6.7 μM.

Download Inhibitor Catalog

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)

References

Solubility (25°C)

In vitro	Ethanol	42 mg/mL (100.39 mM)
	Water	35 mg/mL (83.66 mM)
	DMSO	28 mg/mL (66.92 mM)

Chemical Information

Molecular Weight	418.36
Formula	C₂₂H₂₄ClN₃O.HCl
CAS No.	79307-93-0
Storage	3 years	-20°C	powder
Storage	2 years	-80°C	in solvent
Smiles	CN1CCCC(CC1)N2C(=O)C3=CC=CC=C3C(=N2)CC4=CC=C(C=C4)Cl.Cl

Download Azelastine HCl SDF

In vivo Formulation Calculator (Clear solution)

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

Dosage: mg/kg Average weight of animals: g Dosing volume per animal:μL Number of animals:

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
=	×	×

Dilution Calculator Molecular Weight Calculator

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 2022-01-17)

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

C1=C0/X	C1:	LOG(C1):
C2=C1/X	C2:	LOG(C2):
C3=C2/X	C3:	LOG(C3):
C4=C3/X	C4:	LOG(C4):
C5=C4/X	C5:	LOG(C5):
C6=C5/X	C6:	LOG(C6):
C7=C6/X	C7:	LOG(C7):
C8=C7/X	C8:	LOG(C8):