Azelastine HCl
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MedKoo CAT#: 317302

CAS#: 79307-93-0

Description: Azelastine HCl is a potent and selective H1-receptor antagonist, with antiallergic effects related to histamine antagonism, and further antiallergic and anti-inflammatory effects unrelated to H1-receptor binding. Azelastine HCl is an activator of NF-kB activator. Azelastine hydrochloride has been used in a study to investigate the potential of polymeric microspheres for treatment of allergic conjunctivitis. Azelastine is shown to block secretion of IL-6, IL-8, and TNF alpha from mast cells by inhibiting NF-κB activation.


Chemical Structure

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Azelastine HCl
CAS# 79307-93-0

Theoretical Analysis

MedKoo Cat#: 317302
Name: Azelastine HCl
CAS#: 79307-93-0
Chemical Formula: C22H25Cl2N3O
Exact Mass:
Molecular Weight: 418.36
Elemental Analysis: C, 63.16; H, 6.02; Cl, 16.95; N, 10.04; O, 3.82

Price and Availability

Size Price Availability Quantity
500.0mg USD 600.0 2 Weeks
1.0g USD 960.0 2 Weeks
2.0g USD 1550.0 2 Weeks
5.0g USD 2850.0 2 Weeks
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Synonym: Azelastine HCl; Astelin; Optivar; Allergodil; Rhinolast; Azeptin

IUPAC/Chemical Name: 4-[(4-chlorophenyl)methyl]-2-(1-methylazepan-4-yl)phthalazin-1-one;hydrochloride

InChi Key: YEJAJYAHJQIWNU-UHFFFAOYSA-N

InChi Code: 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

SMILES Code: CN1CCCC(CC1)N2C(=O)C3=CC=CC=C3C(=N2)CC4=CC=C(C=C4)Cl.Cl

Appearance: Solid powder

Purity: >98% (or refer to the Certificate of Analysis)

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.

Storage Condition: Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).

Solubility: Soluble in DMSO, not in water

Shelf Life: >2 years if stored properly

Drug Formulation: This drug may be formulated in DMSO

Stock Solution Storage: 0 - 4 C for short term (days to weeks), or -20 C for long term (months).

HS Tariff Code: 2934.99.9001

Preparing Stock Solutions

The following data is based on the product molecular weight 418.36 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Recalculate based on batch purity %
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 1.15 mL 5.76 mL 11.51 mL
5 mM 0.23 mL 1.15 mL 2.3 mL
10 mM 0.12 mL 0.58 mL 1.15 mL
50 mM 0.02 mL 0.12 mL 0.23 mL

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1: El-Shaheny RN, Yamada K. Stability study of the antihistamine drug azelastine
HCl along with a kinetic investigation and the identification of new degradation
products. Anal Sci. 2014;30(6):691-7. PubMed PMID: 24919676.

2: Meltzer EO, Garadi R, Laforce C, Chadwick SJ, Berger WE, Gross G, Edwards MR,
Crenshaw K, Wall GM. Comparative study of sensory attributes of two antihistamine
nasal sprays: olopatadine 0.6% and azelastine 0.1%. Allergy Asthma Proc. 2008
Nov-Dec;29(6):659-68. doi: 10.2500/aap.2008.29.3181. Epub 2008 Dec 6. PubMed
PMID: 19144261.

3: Alberty J, Stoll W. The effect of antiallergic intranasal formulations on
ciliary beat frequency of human nasal epithelium in vitro. Allergy. 1998
Oct;53(10):986-9. PubMed PMID: 9821480.

4: Morganroth J, Lyness WH, Perhach JL, Mather GG, Harr JE, Trager WF, Levy RH,
Rosenberg A. Lack of effect of azelastine and ketoconazole coadministration on
electrocardiographic parameters in healthy volunteers. J Clin Pharmacol. 1997
Nov;37(11):1065-72. PubMed PMID: 9506001.

5: Bussi M, Carlevato MT, Majore L, Battaglio S, Napoli P, Cortesina G. [The
problem of recurrence of rhino-sinusal polyposis: pilot trial with locally
administered azelastine HCL in the prevention of relapses]. Acta Otorhinolaryngol
Ital. 1995 Apr;15(2):101-6. Italian. PubMed PMID: 8928647.

6: Conde Hernández J, Palma Aguilar JL, Delgado Romero J. Investigation on the
efficacy and tolerance of azelastine (HCL) nasal spray versus ebastine tablets in
patients with seasonal allergic rhinitis. Allergol Immunopathol (Madr). 1995
Mar-Apr;23(2):51-7. PubMed PMID: 8526167.

7: Leitch IM, Temple DM, Wei H, Boura AL. Some anti-allergic and
anti-inflammatory actions of 2-N-carboxamidinonormianserin (FCC5). J Pharm
Pharmacol. 1995 Feb;47(2):143-7. PubMed PMID: 7541457.

8: Matsui C, Ida M, Hamada M, Morohashi M, Hasegawa M. Effects of azelastin on
pruritus and plasma histamine levels in hemodialysis patients. Int J Dermatol.
1994 Dec;33(12):868-71. PubMed PMID: 7883414.

9: Langevin CN, Pivonka J, Wichmann JK, Kucharczyk N, Sofia RD. High performance
liquid chromatographic determination of azelastine and desmethylazelastine in
guinea pig plasma and lung tissue. Biomed Chromatogr. 1993 Jan-Feb;7(1):7-11.
PubMed PMID: 8094306.

10: Kietzmann M, Lubach D, Molliere M, Szelenyi I. Effects of the phthalazinone
azelastine on epidermal metabolism after mechanical skin irritation.
Pharmacology. 1992;45(5):269-77. PubMed PMID: 1361235.

11: Ulbrich E, Nowak H. Long-term multicentric study with azelastine in patients
with intrinsic asthma. Arzneimittelforschung. 1990 Nov;40(11):1225-30. PubMed
PMID: 2085334.

12: Komatsu H, Takehana Y, Kikuchi S, Kojima M, Hamano S, Kusama H, Okegawa T,
Ikeda S. Effect of a thromboxane A2 synthetase inhibitor (OKY-046.HCl) on airway
hyperresponsiveness in guinea pigs. Eur J Pharmacol. 1990 Aug 2;184(1):87-95.
PubMed PMID: 2170151.

13: Kurosawa M, Okayama Y, Kobayashi S. Inhibitory effect of adenine nucleotides
and anti-allergic drugs on phosphorylation of phosphatidylinositol in rat mast
cell granules. Allergy. 1989 Nov;44(8):576-81. PubMed PMID: 2575358.

14: Shibata N, Akagami H, Sanma H, Goshima K. Augmentation of eicosanoids in
ischemic heart muscle in dogs: its role in the deterioration of the ischemic
lesion. Jpn Circ J. 1988 Jul;52(7):673-83. PubMed PMID: 3141656.