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Respiratory, allergy and digestive drugs

Azelastine

Also known as Azelastina, 4-(4-chlorobenzyl)-2-(1-methylazepan-4-yl)phthalazin-1(2H)-one, Azelastinum

CAS 58581-89-8Formula C22H24ClN3OMolar mass 381.91 g/molEC 611-699-2
GHS signal word: Warning. Pictograms: Harmful or irritant, Serious health hazard 81 suppliers listed Drug substance
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Azelastine chemical structure, C22H24ClN3O, CAS 58581-89-8
2D chemical structure

Key facts

What buyers check first

All properties
CAS number
58581-89-8
Formula
C22H24ClN3O
Appearance
Oil
Solubility
Soluble in methylene chloride
HS code
293399
Category
Respiratory, allergy and digestive drugs
Illustrative photo, 200 litre steel drums of liquid in a chemical plant
Typical packagingIllustrative packaging image, not the actual product

What is Azelastine?

Plain description, key identifiers and synonyms

Azelastine is a phthalazine compound having an oxo substituent at the 1-position, a 1-methylazepan-4-yl group at the 2-position and a 4-chlorobenzyl substituent at the 4-position. It has a role as a bronchodilator agent, a H1-receptor antagonist, an anti-asthmatic drug, a platelet aggregation inhibitor, an anti-allergic agent and an EC 1.13.11.34 (arachidonate 5-lipoxygenase) inhibitor. It is a member of phthalazines, a tertiary amino compound and a member of monochlorobenzenes.

Identifiers

Registry numbers, names and line notations, tap to copy

IUPAC name
4-[(4-chlorophenyl)methyl]-2-(1-methylazepan-4-yl)phthalazin-1-one
CAS number
58581-89-8 CAS number cross-checkedOther or deprecated CAS: 758637-88-6
EC number
611-699-2
Molecular formula
C22H24ClN3O
UNII
ZQI909440X
InChIKey
MBUVEWMHONZEQD-UHFFFAOYSA-N
InChI
InChI=1S/C22H24ClN3O/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
SMILES (canonical and isomeric)
CN1CCCC(CC1)N2C(=O)C3=CC=CC=C3C(=N2)CC4=CC=C(C=C4)Cl

Synonyms

  • Azelastina
  • 4-(4-chlorobenzyl)-2-(1-methylazepan-4-yl)phthalazin-1(2H)-one
  • Azelastinum
  • 4-(p-Chlorobenzyl)-2-(hexahydro-1-methyl-1H-azepin-4-yl)-1-(2H)-phthalazinone
  • 1(2H)-Phthalazinone, 4-((4-chlorophenyl)methyl)-2-(hexahydro-1-methyl-1H-azepin-4-yl)-
  • 4-[(4-chlorophenyl)methyl]-2-(1-methylazepan-4-yl)-1,2-dihydrophthalazin-1-one
  • 4-((4-chlorophenyl)methyl)-2-(1-methylazepan-4-yl)-1,2-dihydrophthalazin-1-one
  • Vividrin akut Azelastin
  • 4-(p-chlorobenzyl)-2-(N-methylperhydroazepinyl-(4))-1-(2H)-phthalazinone
  • 4-[(4-chlorophenyl)methyl]-2-(1-methylazepan-4-yl)phthalazin-1-one
  • Azelastine (INN)
  • Optilast
  • 1(2H)-Phthalazinone,4-[(4-chlorophenyl)methyl]-2-(hexahydro-1-methyl-1H-azepin-4-yl)-
  • 4-((4-Chlorophenyl)methyl)-2-(hexahydro-1-methyl-1H-azepin-4-yl)-1(2H)-phthalazinone hydrochloride
  • 4-[(4-chlorophenyl)methyl]-2-(1-methylazepan-4-yl)phthalazin-1(2H)-one
  • 1(2H)-phthalazinone, 4-[(4-chlorophenyl)methyl]-2-(hexahydro-1-methyl-1H-azepin-4-yl)-, hydrochloride
  • Optivar (TN)
  • rac-Azelastine
  • 4-[(4-Chlorophenyl)methyl]-2-(hexahydro-1-methyl-1H-azepin-4-yl)-1(2H)-phthalazinone,
  • (+-)-Azelastine
  • 1(2H)-phthalazinone,4-[(4-chlorophenyl)methyl]-2-[(4s)-hexahydro-1-methyl-1h-azepin-4-yl]-

Physical and chemical properties

Measured values and descriptors computed from the structure

Physical and chemical properties

Measured values, check the supplier specification for your grade

Appearance
Oilexp.
Solubility
Soluble in methylene chlorideexp.

Values vary by grade. Ask suppliers for the COA or TDS of the batch you buy.

Computed descriptors

Calculated from the structure, useful for screening and formulation

Molecular weight
381.91 g/molcalc.
Exact mass
381.1608 Dacalc.
LogP (octanol/water)
4.3calc.
Topological polar surface area
38.13 Ųcalc.
Hydrogen bond donors
0calc.
Hydrogen bond acceptors
3calc.
Rotatable bonds
3calc.
Heavy atoms
27calc.
Rings
4calc.
Aromatic rings
3calc.
Fraction sp3 carbons
0.36calc.
Formal charge
0calc.
Stereocentres
1calc.
Lipinski rule of five
Passes (0 violations)calc.

Calculated for screening. Confirm critical figures with the supplier.

Murcko scaffold

The ring system that remains when every side chain is removed

Murcko scaffold of this chemical, O=c1c2ccccc2c(Cc2ccccc2)nn1C1CCCNCC1

O=c1c2ccccc2c(Cc2ccccc2)nn1C1CCCNCC1

4 rings, 25 atoms.

21 other chemicals share this scaffold

Safety and hazards

GHS classification summary, not a safety data sheet

GHS signal word
Warning
GHS07: Harmful or irritant
Harmful or irritant
GHS08: Serious health hazard
Serious health hazard

Hazard statements

  • H302Harmful if swallowed.
  • H312Harmful in contact with skin.
  • H315Causes skin irritation.
  • H332Harmful if inhaled.
  • H335May cause respiratory irritation.
  • H351Suspected of causing cancer.
  • H413May cause long lasting harmful effects to aquatic life.
Precautionary statements (20)
  • P203Obtain, read and follow all safety instructions before use.
  • P261Avoid breathing dust, fume, gas, mist, vapours or spray.
  • P264Wash skin thoroughly after handling.
  • P270Do not eat, drink or smoke when using this product.
  • P271Use only outdoors or in a well-ventilated area.
  • P273Avoid release to the environment.
  • P280Wear protective gloves, protective clothing, eye protection and face protection.
  • P301 + P317If swallowed: Get medical help.
  • P302 + P352If on skin: Wash with plenty of water.
  • P304 + P340If inhaled: Remove person to fresh air and keep comfortable for breathing.
  • P317Get medical help.
  • P318If exposed or concerned, get medical advice.
  • P319Get medical help if you feel unwell.
  • P321Specific treatment (see supplemental first aid instructions on the label).
  • P330Rinse mouth.
  • P332 + P317If skin irritation occurs: Get medical help.
  • P362 + P364Take off contaminated clothing. And wash it before reuse.
  • P403 + P233Store in a well-ventilated place. Keep container tightly closed.
  • P405Store locked up.
  • P501Dispose of contents and container in accordance with local regulations.

GHS classification summary, not a safety data sheet (SDS). Classifications can differ by supplier, grade and concentration. Always check the supplier's SDS.

Full safety data and first aid

Azelastine suppliers

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All 81 suppliers
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Where suppliers are based

81 suppliers in 15 countries

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Azelastine price

Indicative price range per kg from live supplier offers

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Uses and applications

What the substance is used for, by industry and function

Pharmacological actions

  • Anti-Allergic Agents
  • Bronchodilator Agents
  • Histamine H1 Antagonists, Non-Sedating
  • Lipoxygenase Inhibitors

Roles

  • H1-receptor antagonist
  • antagonist
  • anti-allergic agent
  • anti-asthmatic agent
  • anti-asthmatic drug
  • bronchodilator agent
  • enzyme inhibitor
  • hematologic agent
  • histamine antagonist
  • histaminergic drug
  • lipoxygenase inhibitor
  • nasal decongestant
  • neurotransmitter agent
  • pharmaceutical
  • platelet aggregation inhibitor

Pharmacology

Azelastine is a Histamine-1 Receptor Antagonist. The mechanism of action of azelastine is as a Histamine H1 Receptor Antagonist.

How it is made

Preparation: BE 778269, D. Vogelsang et al., US 3813384 (1972, 1974 both to Asta-Werke AG)

Regulatory status

Inventories, regulations and trade controls that list this substance

Health and food

  • Active ingredient in FDA approved drug labels

HS code and trade data

Customs classification and reported world trade statistics

Global trade

World import and export statistics for the HS code Azelastine is traded under.

HS 2933.99Indicative HS code

Heterocyclic compounds with nitrogen hetero-atom(s) only, other

World exports in 2024
$12.1B
−31.0% vs 2023, imports $28.8B
2019 to 2024
Top exporters
  1. China30.5%
  2. India * partner reported16.3%
  3. Ireland9.0%
Top importers
  1. Slovenia31.7%
  2. Italy24.2%
  3. United States5.0%

* Partner reported figures, a lower bound.

Reported customs values in USD, not prices.Full trade data

The HS code shown for Azelastine is indicative (it was assigned by structure rules). Confirm the classification with your customs broker before shipping.

Frequently asked questions

Quick answers about Azelastine, based on the data on this page

What is Azelastine?

Azelastine is a phthalazine compound having an oxo substituent at the 1-position, a 1-methylazepan-4-yl group at the 2-position and a 4-chlorobenzyl substituent at the 4-position.

What is the CAS number of Azelastine?

The CAS registry number of Azelastine is 58581-89-8. Other or deprecated CAS numbers: 758637-88-6.

What is the molecular formula and weight of Azelastine?

The molecular formula of Azelastine is C22H24ClN3O and its molar mass is 381.91 g/mol.

What is Azelastine used for?

Known uses and roles of Azelastine include respiratory and anti-allergy drugs in pharmaceuticals, h1-receptor antagonist, antagonist, anti-allergic agent, anti-asthmatic agent and 15 more.

Is Azelastine hazardous?

Azelastine carries the GHS signal word "Warning". Main hazards: harmful if swallowed, harmful in contact with skin, causes skin irritation. This summary is not an SDS, always read the supplier safety data sheet.

What is the HS code of Azelastine?

Azelastine is usually classified under HS code 293399 (Heterocyclic compounds with nitrogen hetero-atom(s) only, other). This is indicative, confirm it with your customs broker before shipping.

Where can I buy Azelastine?

CompoundList lists 81 suppliers of Azelastine in United States, China, India, Hong Kong and 11 more. Send one free request to get and compare quotes. Your contact details stay private until you accept a quote.

Where can I buy Azelastine in India?

13 suppliers in India list Azelastine on CompoundList. Filter the suppliers list by country and send a request to compare prices, grades and delivery times.

What is the price of Azelastine?

Suppliers quote Azelastine on request because prices depend on grade, purity, quantity and destination. A free request on CompoundList gets you several quotes to compare.

Guides for buyers

Practical guides that help when you source, ship or handle Azelastine

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Data last updated 7 Oct 2026. Details may have changed, please confirm them with the supplier. Report an error on this page
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