EMEDASTINE FUMARATE

ChemicalBook > CAS DataBase List > EMEDASTINE FUMARATE

Product Name: EMEDASTINE FUMARATE
CAS No.: 87233-62-3
Chemical Name: EMEDASTINE FUMARATE
Synonyms: Emadine;1-(2-ethoxyethyl)-2-(4-methyl-1-homopiperazinyl)benzimidazoledifumarate;Daren;kb2413;Remicut;kb-2413;kg-2413;Rapimine;AL 3432A;ly188695
CBNumber: CB6714475
Molecular Formula: C25H34N4O9
Formula Weight: 534.56
MOL File: 87233-62-3.mol

Less

EMEDASTINE FUMARATE Property

Melting point:: 148-151°
storage temp.: 2-8°C
solubility: Soluble in water, sparingly soluble in anhydrous ethanol, very slightly soluble in acetone.
Merck: 14,3557

Less

Safety

RTECS: DD8870000
HS Code: 2933992600
Toxicity: LD50 orally in guinea pigs: 744 mg/kg (Fukuda)

Less

Hazard and Precautionary Statements (GHS)

Symbol(GHS)

Signal word

Warning

Hazard statements

H302Harmful if swallowed

Precautionary statements

P264Wash hands thoroughly after handling.

P264Wash skin thouroughly after handling.

P270Do not eat, drink or smoke when using this product.

P501Dispose of contents/container to..…

Less

N-Bromosuccinimide Price

Sigma-Aldrich

Product number: Y0000537
Product name: Emedastine difumarate
Purity: European Pharmacopoeia (EP) Reference Standard
Packaging: y0000537
Price: $150
Updated: 2024/03/01

Sigma-Aldrich

Product number: 1234806
Product name: Emedastine difumarate
Packaging: 100mg
Price: $406
Updated: 2024/03/01

TCI Chemical

Product number: E0936
Product name: Emedastine Difumarate
Purity: >98.0%(HPLC)(T)
Packaging: 200mg
Price: $244
Updated: 2021/12/16

Cayman Chemical

Product number: 23946
Product name: Emedastine (fumarate)
Purity: ≥98%
Packaging: 5mg
Price: $32
Updated: 2024/03/01

Cayman Chemical

Product number: 23946
Product name: Emedastine (fumarate)
Purity: ≥98%
Packaging: 10mg
Price: $61
Updated: 2024/03/01

Less

EMEDASTINE FUMARATE Chemical Properties,Usage,Production

Description

Emedastine difumarate, a potent H₁-receptor antagonist, was launched in Japan for the treatment of allergic rhinitis and urticaria. Emedastine exerts its antiallergic effect via inhibition of substance P-induced histamine release. It has been demonstrated both in vitro and in vivo that this effect is mediated by the inhibition of Ca²⁺release from extracellular stores and of Ca²⁺ influx into mast cells. In a clinical trial with bronchial asthma, emedastine improved asthmatic symptoms in 55.3% of patients.

Description

Emedastine is a histamine H₁ receptor antagonist (K_i = 1.3 nM). It is selective for histamine H₁ over H₂ and H₃ receptors (K_is = 49 and 12.43 μM, respectively), as well as α₁-, α₂-, and β₁-adrenergic and dopamine D₁ and D₂ receptors, and the serotonin (5-HT) receptor subtypes 5-HT₁ and 5-HT₂ at 10 μM. Emedastine inhibits histamine-induced phosphoinositide turnover and intracellular calcium mobilization in primary human conjunctival epithelial cells (HCECs; IC₅₀s = 1.6 and 2.9 nM, respectively). It also inhibits histamine-stimulated secretion of IL-6, IL-8, and GM-CSF by primary HCECs (IC₅₀s = 2.23, 3.42, and 1.50 nM, respectively). Ocular application of emedastine prior to histamine challenge inhibits vascular permeability in guinea pigs. Formulations containing emedastine have been used in the treatment of allergic conjunctivitis.

Chemical Properties

White or yellowish powder

Originator

Kanebo (Japan)

Uses

Antihistaminic, H1-receptor; asthma prophylactic; anti-allergic.

Definition

ChEBI: The fumaric acid salt of emedastine containing two molecules of fumaric acid for each molecule of emedastine. A relatively selective histamine H1 antagonist, it is used for allergic rhinitis, urticaria, and pruritic skin disorders, and in eyedrops for the symptomatic relief of allergic conjuntivitis.

Manufacturing Process

Preparation of 2-(4-methyl-1-piperazinyl)benzimidazole. A mixture of 2- chlorobenzimidazole (10.00 g) and N-mehylpiperazine (20.00 g) is stirred at 125°C for 5 hours. A 10% aqueous sodium hydroxide (100 ml) is added to the reaction mixture, and the precipitated crystals are separated by filtration. The filtrate is extracted with chloroform, and the chloroform extract is evaporated to dryness to give the same crystals. The crystals are combined and recrystallized from water-methanol to give 2-(4-methyl-1- piperazinyl)benzimidazole (7.02 g) as colorless needles, m.p. 225°-226°C.
2-(4-Methyl-1-piperazinyl)benzimididazole (5.00 g) prepared as above is dissolved in N,N-dimethylformamide (50 ml) and thereto is added sodium hydride (concentration: 50%) (1.50 g) at room temperature, and the mixture is stirred for 30 minutes. To the mixture is added 2-bromoethyl ethyl ether (4.00 g), and the mixture is stirred at 70°C for 10 hours. To the reaction mixture is added water (150 ml), and the mixture is extracted with ethyl acetate. The extract is washed with water, dried over anhydrous magnesium sulfate and then concentrated to give a brown oily substance (5.40 g). The brown oily substance is treated with fumaric acid (3.26 g) in hot ethanol. The crude crystals thus obtained are recrystallized from ethyl acetate-ethanol to give 1-[2-(ethoxy)ethyl]-2-(4-methyl-1-piperazinyl)benzimidazole 3/2 fumarate (6.31 g) as colorless plates, melting point 167.5°-168.5°C. Elementary analysis for C22H30N4O7: Calcd. (%): C, 57.13; H, 6.54; N, 12.11; Found (%): C, 57.04; H, 6.44; N, 12.02.
1-[2-(Ethoxy)ethyl]-2-(4-methyl-1-piperazinyl)benzimidazole can be prepared using 2-chloro-(1-[2-(ethoxy)ethyl]benzimidazole), (last one can be produced from 2-bromoethyl ethyl ether 2-chlorobenzimidazole) and N-methylpiperazine and fumaric acid there are obtained crude crystals, which are recrystallized from ethanol to give 1-[2-(ethoxy)ethyl]-2-(4-methyl-1- piperazinyl)benzimidazole 3/2 fumarate. This product has the same physical properties as those of the product above described.

brand name

Emadine (Alcon);Daren;Remicut.

Therapeutic Function

Antiallergic, Antihistaminic

Hazard

A poison by ingestion.

EMEDASTINE FUMARATE Preparation Products And Raw materials

Raw materials

Preparation Products

Less

EMEDASTINE FUMARATE Suppliers

China 112 Europe 1 France 1 India 5 South Korea 1 United Kingdom 1 United States 15 Global 136

NanJing Vtrying Pharmatech Co.,Ltd

Tel: 17314186806
Email: Vtrying_sale@163.com
Country: China
ProdList: 89
Advantage: 58

NANJING TOMMLAB PHARMATECH Co.,LTD

Tel: --
Fax: --
Email: litianang@caremo.com.cn
Country: China
ProdList: 271
Advantage: 58

Shanghai Boyle Chemical Co., Ltd.

Tel
Fax: 86-21-57758967
Email: sales@boylechem.com
Country: China
ProdList: 2922
Advantage: 55

J & K SCIENTIFIC LTD.

Tel: 010-82848833 400-666-7788
Fax: 86-10-82849933
Email: jkinfo@jkchemical.com
Country: China
ProdList: 96815
Advantage: 76

TCI (Shanghai) Development Co., Ltd.

Tel: 021-67121386
Fax: 021-67121385
Email: Sales-CN@TCIchemicals.com
Country: China
ProdList: 24529
Advantage: 81

Shanghai Yuanding Chem. Sci. & Tech. Co., Ltd.

Tel: 21-57721279
Fax: QQ：14057904
Email: sales@shydchem.com.cn
Country: China
ProdList: 990
Advantage: 56

Adamas Reagent, Ltd.

Tel: 400-6009262 16621234537
Fax: 021-64823266
Email: chenyj@titansci.com
Country: China
ProdList: 14103
Advantage: 59

XiaoGan ShenYuan ChemPharm co,ltd

Tel: 15527768850
Email: 1791901229@qq.com
Country: China
ProdList: 8837
Advantage: 52

Sinopharm Chemical Reagent Co,Ltd.

Tel: 86-21-63210123
Fax: 86-21-63290778 86-21-63218885
Email: sj_scrc@sinopharm.com
Country: China
ProdList: 9815
Advantage: 79

Hunan Hui Bai Shi Biotechnology Co., Ltd.

Tel: 0731-85526065 13308475853
Email: ivy@hnhbsj.com
Country: China
ProdList: 4554
Advantage: 62

9ding chemical ( Shanghai) Limited

Tel: 4009209199
Fax: 86-021-52271987
Email: sales@9dingchem.com
Country: China
ProdList: 22514
Advantage: 55

Shanghai Aladdin Bio-Chem Technology Co.,LTD

Tel: 400-400-6206333 18521732826
Fax: 021-50323701
Email: market@aladdin-e.com
Country: China
ProdList: 25003
Advantage: 65

TargetMol Chemicals Inc.

Tel: 021-021-33632979 15002134094
Fax: 021-33632979
Email: marketing@targetmol.com
Country: China
ProdList: 7783
Advantage: 58

ChemStrong Scientific Co.,Ltd

Tel: 0755-0755-66853366 13670046396
Fax: 0755-28363542
Email: sales@chem-strong.com
Country: China
ProdList: 18070
Advantage: 56

Shanghai Synteam Biochem CO.,ltd

Tel: +86-021-58380978 +86-18017016373
Fax: 021-58380978
Email: info@systeambc.com
Country: China
ProdList: 942
Advantage: 50

Jiangsu Aikon Biopharmaceutical R&D co.,Ltd.

Tel: 025-66113011 18112977050
Email: cb6@aikonchem.com
Country: China
ProdList: 16684
Advantage: 50

Chizhou Kailong Import and Export Trade Co., Ltd.

Tel
Fax: -
Email: xg01_gj@163.com
Country: China
ProdList: 9484
Advantage: 50

Nanjing XiZe Biotechnology CO., Ltd.

Tel: 025-66023220 0086-15250997978
Fax: 025-58362220
Email: 1511893459@qq.com
Country: China
ProdList: 7850
Advantage: 55

Taizhou Elitechemie MediPharma Technology Co., Ltd.

Tel: 523-86810021 18921709486
Fax: gwli@elitechemie.com
Email: gwli@elitechemie.com
Country: China
ProdList: 507
Advantage: 65

Shanghai QianYan Bio-technology Co., Ltd

Tel: 02781293128
Email: orders@biochemsafebuy.com
Country: China
ProdList: 9923
Advantage: 55

Raw material medicin reagent co.,Ltd

Tel
Email: sales@njromanme.com
Country: China
ProdList: 4529
Advantage: 58

Chengdu Dianchun Technology Co., Ltd

Tel: 400-1166-196 18502815961
Fax: QQ：800101999
Email: cdhxsj@163.com
Country: China
ProdList: 14603
Advantage: 60

Beijing Solarbio Science & Tecnology Co., Ltd.

Tel: 010-50973186 4009686088
Email: 3193328036@qq.com
Country: China
ProdList: 18338
Advantage: 68

Hubei widely chemical technology Co., Ltd.

Tel: 027-83991130 18627774460
Fax: 027-83991130
Email: 1718093273@QQ.COM
Country: China
ProdList: 1880
Advantage: 58

Hubei widely chemical technology Co., Ltd.

Tel: 027-59402396 13419635609
Fax: 027-83989310
Email: 13419635609@163.com
Country: China
ProdList: 1984
Advantage: 55

Wuhan Wsem Biological Co., Ltd.

Tel: 027-83778876 13667159345
Fax: 027-83778876
Email: 13667159345@163.com
Country: China
ProdList: 1996
Advantage: 55

Wellman Pharmaceutical Group Limited

Tel: 027-83778875 15807197853
Fax: 027-83991220
Email: 15807197853@163.com
Country: China
ProdList: 4026
Advantage: 58

9ding chemical ( Shanghai) Limited

Tel: 021-021-52271985 17721149837
Fax: +86 (21) 52271987
Email: sales@9dingchem.com
Country: China
ProdList: 19800
Advantage: 60

Zhaoqing Wanwei New Material Technology Co., Ltd.

Tel: 0755-1328880-4488 13068786899
Fax: 13068786899
Email: 13288804488@163.com
Country: China
ProdList: 625
Advantage: 58

Hubei Xinyuanshun Pharmaceutical Chemical Co., Ltd.

Tel: 027-51831887 15337167856
Fax: 027-51837635 QQ1165326703
Email: hubeixinyuanshun@163.com
Country: China
ProdList: 10295
Advantage: 58

Chengdu Saint - Kay Biotechnology Co., Ltd.

Tel: 028-85157043 15882256948
Email: 676046971@qq.com
Country: China
ProdList: 4394
Advantage: 58

Shanghai Jizhi Biochemical Technology Co. Ltd.

Tel: 4009004166/18616739031 18616739031
Email: 3007523370@qq.com
Country: China
ProdList: 52693
Advantage: 58

Shanghai Hongye Biotechnology Co. Ltd

Tel: 400-9205774
Email: sales@glpbio.cn
Country: China
ProdList: 6777
Advantage: 58

Shenzhen Polymeri Biochemical Technology Co., Ltd.

Tel: +86-400-002-6226 +86-13028896684;
Email: sales@rrkchem.com
Country: China
ProdList: 57423
Advantage: 58

Guangzhou Tomums Life Science Co., Ltd.

Tel: 020-31155029 18902330969
Fax: 020-31155029
Email: sales@tomums.cn
Country: China
ProdList: 4696
Advantage: 58

Hefei TNJ Chemical Industry Co.,Ltd.

Tel: +86-0551-65418684 +8618949823763
Fax: 0086-551-65418684
Email: sales@tnjchem.com
Country: China
ProdList: 25356
Advantage: 58

Hebei Zhanyao Biotechnology Co. Ltd

Tel: 15369953316 +8615369953316
Email: admin@zhanyaobio.com
Country: China
ProdList: 2123
Advantage: 58

Dayang Chem (Hangzhou) Co.,Ltd.

Tel: 571-88938639 +8617705817739
Fax: +86-571-88938652，+86-571- 88492614
Email: info@dycnchem.com
Country: China
ProdList: 52849
Advantage: 58

Baoji Guokang Bio-Technology Co., Ltd.

Tel: 0917-3909592 13892490616
Fax: 09173909592
Email: gksales1@gk-bio.com
Country: China
ProdList: 9312
Advantage: 58

Baoji Guokang Healthchem co.,ltd

Tel: +8615604608665 15604608665
Email: dominicguo@gk-bio.com
Country: CHINA
ProdList: 9414
Advantage: 58

AFINE CHEMICALS LIMITED

Tel: +86-0571-85134551
Fax: 008657185134895
Email: sales@afinechem.com
Country: China
ProdList: 15352
Advantage: 58

Career Henan Chemica Co

Tel: +86-0371-86658258 +8613203830695
Fax: 0371-86658258
Email: laboratory@coreychem.com
Country: China
ProdList: 30239
Advantage: 58

Hubei Xingcheng Biotechnology Co., Ltd

Tel: 19171210221
Fax: QQ:3505191060
Email: 3371991952@qq.com
Country: China
ProdList: 957
Advantage: 58

Chemwill Asia Co.,Ltd.

Tel: 86-21-51086038
Fax: 86-21-51861608
Email: chemwill_asia@126.com
Country: CHINA
ProdList: 23912
Advantage: 58

Guangdong Wengjiang Chemical Reagent Co., Ltd.

Tel: 0751-2886766 13927870850
Fax: 0751-2886756
Email: 3001267247@qq.com
Country: China
ProdList: 9974
Advantage: 58

Jinan blalong chemical co. LTD

Tel: 2710913286@.com
Email: 1513643261@qq.com
Country: China
ProdList: 14246
Advantage: 58

ChemeGen(Shanghai) Biotechnology Co.,Ltd.

Tel: 18818260767
Fax: QQ 3610331285
Email: sales@chemegen.com
Country: China
ProdList: 11218
Advantage: 58

Hubei widely chemical technology Co., Ltd.

Tel: 027-83989310 18627915365
Fax: 027-83989310
Email: 2658488909@qq.com
Country: China
ProdList: 1297
Advantage: 58

Shaanxi Dideu Medichem Co. Ltd

Tel: +86-29-87569266 15319487004
Fax: 029-88380327
Email: 1015@dideu.com
Country: China
ProdList: 3943
Advantage: 58

Shanghai hongqu biomedical technology co. LTD

Tel: 88888888888
Email: hongquchem@qq.com
Country: China
ProdList: 5132
Advantage: 58

Less

View Lastest Price from EMEDASTINE FUMARATE manufacturers

Henan Fengda Chemical Co., Ltd

Product: EMEDASTINE FUMARATE 87233-62-3
Price: US $32.00-1.30/KG
Min. Order: 1KG
Purity: 99%
Supply Ability: g-kg-tons, free sample is available
Release date: 2024-04-15

Baoji Guokang Healthchem co.,ltd

Product: EMEDASTINE FUMARATE 87233-62-3
Price: US $150.00/g
Min. Order: 1g
Purity: 99%
Supply Ability: 100KG
Release date: 2021-06-03

Hebei Zhanyao Biotechnology Co. Ltd

Product: EMEDASTINE FUMARATE 87233-62-3
Price: US $10.00/Kg/Bag
Min. Order: 1Kg/Bag
Purity: 99%
Supply Ability: 20 Tons
Release date: 2021-11-22

87233-62-3, EMEDASTINE FUMARATERelated Search:

/ EmedastineN-Oxide Emedastine EP Impurity C HCl EMEDASTINE FUMARATE Emedastine

1-(2-ethoxyethyl)-2-(4-methyl-1-homopiperazinyl)benzimidazoledifumarate

1-(2-ethoxyethyl)-2-(4-methylhexahydro-1h-1,4-diazepin-1-yl)-benzimidazol

1-(2-ethoxyethyl)-2-(4-methylhexahydro-1h-1,4-diazepin-1-yl)benzimidazolefum

1-(2-Ethoxyethyl)-2-(4-methylhexahydro-1H-1,4-diazepine-1-yl)-1H-benzimidazole·bisfumaric acid

Daren

Emedastin difumarate

Emedastin fumarate

Remicut

Emedastine Difumarate (100 mg)

Rapimine

Emadine

AL 3432A

1-(2-Ethoxyethyl)-2-(hexahydro-4-methyl-1H-1,4-diazepin-1-yl)-1H-benzimidazole (2E)-2-butenedioate (1:2)

1-(2-ethoxyethyl)-2-(4-methyl-1,4-diazepan-1-yl)-1H-benzo[d]imidazole difumarate

1h-benzimidazole,1-(2-ethoxyethyl)-2-(hexahydro-4-methyl-1h-1,4-diazepin-1-yl)

arate(1:2)

emedastinedifumarate

kb2413

kb-2413

kg-2413

ly188695

EMEDASTINE FUMARATE

EmedastineDifumarate&gt

Emedastine difumarate CRS

1-(2-Ethoxyethyl)-2-(4-methylhexahydro-1H-1,4-diazepin-1- yl)-1H-benzimidazole bis[hydrogen (2E)-butenedioate

Emestine Fumarate

Emedastine Difumarate (1234806)

Fmedastine Difumarate

87233-62-3

C25H34N4O9

C17H26N4O2C4H4O4