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A7611

Sigma-Aldrich

Azelastine hydrochloride

≥98% (HPLC)

Synonym(s):

4-[(4-chlorophenyl)methyl]-2-(1-methylazepan-4-yl)phthalazin-1-one hydrochloride, Astelin, Optivar

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About This Item

Empirical Formula (Hill Notation):
C22H24ClN3O · HCl
CAS Number:
79307-93-0
Molecular Weight:
418.36
MDL number:
MFCD00242783
UNSPSC Code:
12352200
PubChem Substance ID:
329770938

Quality Level

100

Assay

≥98% (HPLC)

form

powder

storage condition

desiccated

color

white to off-white

solubility

DMSO: >10 mg/mL

originator

Wallace

storage temp.

−20°C

SMILES string

Cl.CN1CCCC(CC1)N2N=C(Cc3ccc(Cl)cc3)c4ccccc4C2=O

InChI

1S/C22H24ClN3O.ClH/c1-25-13-4-5-18(12-14-25)26-22(27)20-7-3-2-6-19(20)21(24-26)15-16-8-10-17(23)11-9-16;/h2-3,6-11,18H,4-5,12-15H2,1H3;1H

InChI key

YEJAJYAHJQIWNU-UHFFFAOYSA-N

Gene Information

human ... HRH1(3269)

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Application

Azelastine hydrochloride is a H1 histamine receptor antagonist and NF-kB activator. Azelastine hydrochloride has been used in a study to investigate the potential of polymeric microspheres for treatment of allergic conjunctivitis.

Biochem/physiol Actions

H1 histamine receptor antagonist; NF-kB activator.

Features and Benefits

This compound is featured on the Histamine Receptors page of the Handbook of Receptor Classification and Signal Transduction. To browse other handbook pages, click here.
This compound was developed by Wallace. To browse the list of other pharma-developed compounds and Approved Drugs/Drug Candidates, click here.

Pictograms

Exclamation mark
GHS07

Signal Word

Warning

Hazard Statements

H302

Precautionary Statements

P264 - P270 - P301 + P312 - P501

Hazard Classifications

Acute Tox. 4 Oral

Storage Class Code

11 - Combustible Solids

Flash Point(F)

Not applicable

Flash Point(C)

Not applicable

Certificates of Analysis (COA)

Search for Certificates of Analysis (COA) by entering the products Lot/Batch Number. Lot and Batch Numbers can be found on a product’s label following the words ‘Lot’ or ‘Batch’.

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Warner Carr et al.
The Journal of allergy and clinical immunology, 129(5), 1282-1289 (2012-03-16)
Moderate-to-severe allergic rhinitis (AR) is a challenge to treat, with many patients using multiple therapies and achieving limited symptom control. More effective therapies must be developed and tested in well-controlled, randomized, prospective studies with a direct comparison to current standards.
Panayiotis A Procopiou et al.
Bioorganic & medicinal chemistry, 20(20), 6097-6108 (2012-09-19)
5-Aza, 6-aza, 7-aza and 8-aza-phthalazinone, and 5,8-diazaphthalazinone templates were synthesised by stereoselective routes starting from the appropriate pyridine/pyrazine dicarboxylic acids by activation with CDI, reaction with 4-chlorophenyl acetate ester enolate to give a β-ketoester, which was hydrolysed, and decarboxylated. The
William C Howland et al.
International forum of allergy & rhinology, 1(4), 275-279 (2012-01-31)
A previous study with azelastine nasal spray in patients with seasonal allergic rhinitis (SAR) demonstrated that increasing the azelastine concentration from 0.1% to 0.15% allowed for once-daily dosing without increasing the incidence of adverse effects. This study evaluated the efficacy
L-L Fu et al.
Cell proliferation, 47(4), 326-335 (2014-06-27)
The aim of this study was to explore sodium taurocholate co-transporting polypeptide (NTCP) exerting its function with hepatitis B virus (HBV) and its targeted candidate compounds, in HBV therapy. Identification of NTCP as a novel HBV target for screening candidate
Eli O Meltzer et al.
Allergy and asthma proceedings, 33(4), 324-332 (2012-08-04)
Many patients with allergic rhinitis (AR) have uncontrolled symptoms despite available treatment options. This study was designed to evaluate the efficacy and safety of MP29-02 (a novel intranasal formulation of fluticasone propionate [FP] and azelastine [AZ] hydrochloride), compared with monotherapy
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