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Azelastine hydrochloride

Product Name
Azelastine hydrochloride
CAS No.
79307-93-0
Chemical Name
Azelastine hydrochloride
Synonyms
AZELASTINE HCL;Astelin;Optivar;1(2H)-Phthalazinone, 4-[(4-chlorophenyl)methyl]-2-(hexahydro-1-methyl-1H-azepin-4-yl)-, monohydrochloride;4-[(4-chlorophenyl)methyl]-2-(hexahydro-1-methyl-1H-azepin-4-yl)-1(2H)-phthalazinone, hydrochloride (1:1);Azen;a5610;e-0659;Azepit;w-2979m
CBNumber
CB9256008
Molecular Formula
C22H25Cl2N3O
Formula Weight
418.36
MOL File
79307-93-0.mol
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Azelastine hydrochloride Property

Melting point:
225--2290C
storage temp. 
Inert atmosphere,Store in freezer, under -20°C
solubility 
DMSO: >10mg/mL
form 
powder
color 
white to off-white
Merck 
14,906
Stability:
Incompatible with strong oxidizing agents.
InChI
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
InChIKey
YEJAJYAHJQIWNU-UHFFFAOYSA-N
SMILES
C1(=O)C2=C(C=CC=C2)C(CC2=CC=C(Cl)C=C2)=NN1C1CCCN(C)CC1.[H]Cl
CAS DataBase Reference
79307-93-0(CAS DataBase Reference)
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Safety

Hazard Codes 
Xn
Risk Statements 
22
RTECS 
TH9203900
HS Code 
2933992600
Toxicity
LD50 in male, female mice, male, female rats (mg/kg): 36.5, 35.5, 26.9, 30.3 i.v.; 56.4, 42.8, 43.2, 46.6 i.p.; 63.0, 54.2, 66.5, 59.6 s.c.; 124, 139, 310, 417 orally (Zechel)
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Hazard and Precautionary Statements (GHS)

Symbol(GHS)
Signal word
Warning
Hazard statements

H302Harmful if swallowed

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N-Bromosuccinimide Price

Sigma-Aldrich
Product number
A7611
Product name
Azelastine hydrochloride
Purity
≥98% (HPLC)
Packaging
10mg
Price
$49.26
Updated
2024/03/01
Sigma-Aldrich
Product number
A7611
Product name
Azelastine hydrochloride
Purity
≥98% (HPLC)
Packaging
50mg
Price
$130.4
Updated
2024/03/01
TCI Chemical
Product number
A2340
Product name
Azelastine Hydrochloride
Purity
>98.0%(HPLC)(T)
Packaging
1g
Price
$187
Updated
2024/03/01
TCI Chemical
Product number
A2340
Product name
Azelastine Hydrochloride
Purity
>98.0%(HPLC)(T)
Packaging
100mg
Price
$37
Updated
2024/03/01
Cayman Chemical
Product number
20873
Product name
Azelastine (hydrochloride)
Purity
≥98%
Packaging
5mg
Price
$36
Updated
2024/03/01
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Azelastine hydrochloride Chemical Properties,Usage,Production

Description

Azelastine hydrochloride is an orally effective antihistamine useful in the treatment of asthma and nasal allergy. It appears to inhibit release of histamine, in addition to antagonizing its action.

Chemical Properties

White or almost white, crystalline powder.

Originator

Asta-Werke(Degussa) (W. Germany)

Uses

Orally active H1-hystamine receptor antagonist. Antihistaminic

Definition

ChEBI: The hydrochloride salt of azelastine.

Application

Azelastine Hydrochloride is the hydrochloride salt form of azelastine, a phthalazinone derivative with antihistaminergic activity. Azelastine hydrochloride exhibits histamine H1-receptor antagonist activity in isolated tissues, animal models, and humans. Azelastine hydrochloride nasal solution is administered as a racemic mixture, and no difference in pharmacologic activity was noted between the enantiomers in vitro studies. The major metabolite, desmethylazelastine, also possesses H1-receptor antagonist activity. It competes with histamine for the H1 receptor, thereby diminishing the actions of histamine on effector cells and decreasing the histamine-mediated symptoms of allergic reaction, such as bronchoconstriction, vasodilation, increased capillary permeability and spasmodic contractions of gastrointestinal smooth muscle.

brand name

Astelin (Medpointe); Optivar (Medpointe);AZEPTIN.

General Description

(±)-4-[(4-chlorophenyl)methyl]-2-(hexahydro-l-methyl-1H-azepin-4-yl)-l-(2H)-phthalazinone monohydrochloride (Optivar), is a whitecrystalline powder that is sparingly soluble in water,methanol, and propylene glycol and slightly soluble inethanol, octanol, and glycerine. The commercial preparationis available as a 0.05% sterile ophthalmic solution fortopical administration to the eyes. Each milliliter of azelastinesolution contains 0.5-mg azelastine hydrochlorideequivalent to 0.457 mg of azelastine base, the preservativebenzalkonium chloride (0.125 mg), and inactive ingredientsincluding disodium edetate dihydrate, hydroxypropylmethylcellulose,sorbitol solution, sodium hydroxide, andwater for injection. The solution has a pH of approximately5.0 to 6.5 and an osmolality of approximately 271to 312 mOsm/L.
The recommended dose of azelastine solution is 1 dropinstilled into each affected eye twice a day. This drugproduct is for ocular administration only and not for injectionor oral use. Absorption of azelastine following ocularadministration is relatively low (less than 1 ng/rnL).Absorbed drug undergoes extensive oxidative N-demethylationby CYP, and the parent drug and metabolite are eliminatedprimarily in the feces. The most frequently reportedadverse reactions are transient eye burning or stinging,headaches, and bitter taste. Azelastine solution should beused with caution during pregnancy or while nursing, becauseits safety has not been studied under these circumstances.

Biochem/physiol Actions

H1 histamine receptor antagonist; NF-kB activator.

Safety Profile

Poison by ingestion andintravenous routes. An experimental teratogen. Otherexperimental reproductive effects. When heated todecomposition it emits toxic fumes of NOx and HCl.

Azelastine hydrochloride Preparation Products And Raw materials

Raw materials

Preparation Products

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View Lastest Price from Azelastine hydrochloride manufacturers

WUHAN FORTUNA CHEMICAL CO., LTD
Product
Azelastine hydrochloride 79307-93-0
Price
US $0.00/g/Bag
Min. Order
100g
Purity
99%min
Supply Ability
300kg/month
Release date
2021-06-05
Shaanxi Dideu Medichem Co. Ltd
Product
Azelastine hydrochloride 79307-93-0
Price
US $1.00-1.00/KG
Min. Order
1g
Purity
99%
Supply Ability
50tons
Release date
2020-05-08
WUHAN CIRCLE POWDER TECHNOLOGY CO.,LTD
Product
Azelastine HCL
Price
US $0.00/KG
Min. Order
100g
Purity
98%+
Supply Ability
100kg
Release date
2021-03-26

79307-93-0, Azelastine hydrochlorideRelated Search:

Basic Violet 1 Topotecan hydrochloride Benzyltrimethylammonium hydroxide Methylparaben Acetonitrile Methyl acrylate Methyl acetate Benzyltriethylammonium chloride Benzyltrimethylammonium chloride Benzyl bromide Benzyl chloride DIBENZYLTOLUENE 1-AdaMantanethylaMine Kresoxim-methyl N,N-Dimethylbenzylamine Methanol Paraquat dichloride Methyl

  • a5610
  • azeptin
  • e-0659
  • w-2979m
  • AZELASTINE HCL
  • AZELASTINE HYDROCHLORIDE
  • 4-[(4-chlorophenyl)methyl]-2-(1-methylazepan-4-yl)-phthalazin-1-one hydrochloride
  • 4-[(4-Chlorophenyl)methyl]-2-(hexahydro-1-methyl-1H-azepin-4-yl)-1(2H)-phthalazinone Hydrochloride
  • Allergodil
  • Astelin
  • Optilast
  • Rhinolast
  • Aselastine
  • 1(2H)-Phthalazinone, 4-[(4-chlorophenyl)methyl]-2-(hexahydro-1-methyl-1H-azepin-4-yl)-, monohydrochloride
  • Acelastine hydrochloride
  • 4-[(4-chlorophenyl)methyl]-2-(hexahydro-1-methyl-1H-azepin-4-yl)-1(2H)-phthalazinone, hydrochloride (1:1)
  • Optivar
  • Adomessen
  • Asutoputin
  • Azen
  • Azepit
  • Azelastine HCI
  • Azelastine-d4 hydrochloride
  • AZWLASTINE HYDROCHLORIDE API
  • 4-(4-Chlorobenzyl)-2-(1-methylazepan-4-yl)-1-phthalazinone Hydrochloride
  • Azelastine hydrochloride (Allergodil)
  • Azelastine-d4 HCl
  • Azelastine HCl (Allergodil)
  • Azelastine hydrochloride CRS
  • Azelastine Hydrochloride &gt
  • 4-hydrazineyl-1-methylazepane hydrogen chloride
  • 4-(4-Chlorobenzyl)-2-[(4RS)-1-methylhexahydro-1H-azepin-4-yl]phthalazin-1(2H)-one hydrochloride
  • Azelastine hydrochloride USP/EP/BP
  • Azelastine hydrochloride (API)
  • Azelastine HydrochlorideQ: What is Azelastine Hydrochloride Q: What is the CAS Number of Azelastine Hydrochloride Q: What is the storage condition of Azelastine Hydrochloride
  • Azelastine Hydrochloride (1046158)
  • 4-[(4-chlorophenyl)methyl]-2-(1-methylazepan-4-yl)-1,2-dihydrophthalazin-1-one hydrochloride
  • 79307-93-0
  • C22H24ClN3OHCl
  • C22H27Cl2N3O
  • C22H25Cl2N3O
  • C22H24ClN3OClH
  • Antihistaminic
  • Astelin
  • Intermediates & Fine Chemicals
  • Pharmaceuticals
  • Histamine receptor