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Acotiamide hydrochloride trihydrate

Product Name
Acotiamide hydrochloride trihydrate
CAS No.
773092-05-0
Chemical Name
Acotiamide hydrochloride trihydrate
Synonyms
Acotiamide hydrochloride hydrate;Acotiamide HCl;Ym-443;Acotiae;Z-338 HCl;YM-443 HCl;Unii-nmw7447A9a;Acofide trihydrate;YM-443;ACOTIAMIDE HCL;Acotiamide trihydrate
CBNumber
CB52493115
Molecular Formula
C21H31ClN4O5S
Formula Weight
487.013
MOL File
773092-05-0.mol
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Acotiamide hydrochloride trihydrate Property

Melting point:
193-195o C
storage temp. 
2-8°C
solubility 
Chloroform (Slightly, Heated, Sonicated), DMSO (Slightly) Methanol (Slightly)
form 
Solid
color 
Pale Yellow
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Hazard and Precautionary Statements (GHS)

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N-Bromosuccinimide Price

TRC
Product number
A190240
Product name
AcofideTrihydrate
Packaging
1g
Price
$210
Updated
2021/12/16
Biosynth Carbosynth
Product number
FA137643
Product name
Acotiamide HCl hydrate
Packaging
500mg
Price
$230
Updated
2021/12/16
Biosynth Carbosynth
Product number
FA137643
Product name
Acotiamide HCl hydrate
Packaging
1g
Price
$350
Updated
2021/12/16
Biosynth Carbosynth
Product number
FA137643
Product name
Acotiamide HCl hydrate
Packaging
2g
Price
$440
Updated
2021/12/16
ChemScene
Product number
CS-0020306
Product name
Acotiamide(monohydrochloridetrihydrate)
Purity
99.28%
Packaging
100mg
Price
$50
Updated
2021/12/16
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Acotiamide hydrochloride trihydrate Chemical Properties,Usage,Production

Description

In June 2013, the Ministry of Health, Labor and Welfare in Japan approved acotiamide (also referred to as Z-338 and YM443), for the treatment of postprandial fullness, upper abdominal bloating, and early satiation due to functional dyspepsia (FD). Acotiamide enhances acetylcholine release from enteric neurons through selective muscarinic acetylcholine receptor M1, M2 antagonism, and inhibition of AChE, thereby enhancing gastric emptying and gastric accommodation. Acotiamide inhibits the acetylcholine-induced Ca2+-activated Cl-current with an IC50 of 1.8 μM in oocytes expressing muscarinic M1 receptors and in oocytes expressing muscarinic M2 receptors, acotiamide inhibited the acetylcholine-induced K+ currents with an IC50 of 10.1 μM. However, studies in conscious dogs, guinea-pig gastric muscle strips and assays with human cholinesterase indicate that acotiamide inhibits AChE with a Ki of 610 nM suggesting that acotiamide stimulates gastric motility mainly by inhibiting AChE activation. In a restraint stress-induced rat model, acotiamide significantly improved delayed gastric emptying and feeding inhibition but did not affect normal gastric emptying or feeding in intact rats. A synthetic route to acotiamide that employs pyridine hydrochloride to selectively cleave a 2-substituted methyl ether from a 2,4,5-trimethoxy benzamide intermediate, as a key step, has been reported.

Originator

Zeria Pharmaceutical (Japan)

Uses

Acofide Trihydrate is a gastrointestinal prokinectic agent used in the treatment of functional malnutrition. A tablet for the treatment of functional dyspepsia.

brand name

Acofide

Synthesis

Commercial 3,4,5-trimethoxybenzoic acid was first converted to the corresponding acid chloride, which was isolated by co-distillation with hexane. In refluxing dichloroethane (DCE), the acid chloride was coupled with the commercially available thiazole amine to give the desired amidothiazole in 89% yield. From this intermediate, amide linkage, selective demethylation of the 2-methoxy group, salt formation, and recrystallization were accomplished in the following sequence: the thiazole ester was reacted with N,N-diisopropyl ethylenediamine in DMA at elevated temperatures. Upon cooling, the mixture was dissolved in n-butanol and washed with aqueous sodium hydroxide. Subsequent treatment with HCl gas in isopropanol gave the corresponding HCl salt as crystals that could be collected by filtration. The product obtained was further crystallized from 4:1 isopropanol and water to give the desired product acotimide (I) as the hydrochloride trihydrate in 71% yield.

Acotiamide hydrochloride trihydrate Preparation Products And Raw materials

Raw materials

Preparation Products

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Acotiamide hydrochloride trihydrate Suppliers

China 213 India 8 South Korea 1 United Kingdom 2 United States 10 Global 234
Anhui Dexinjia Biopharm Co., Ltd
Tel
0531-82375878 15269101859
Email
2710825968@qq.com
Country
China
ProdList
303
Advantage
58
Jinan Rouse Industry Co., Ltd.
Tel
0531-0531-82929600 18615510361
Fax
053182921652
Email
sale@rousechem.com
Country
China
ProdList
176
Advantage
58
Chembest Research Laboratories Limited
Tel
+86-21-20908456
Fax
021-58180499
Email
sales@BioChemBest.com
Country
China
ProdList
6005
Advantage
61
Jia Xing Isenchem Co.,Ltd
Tel
0573-85285100 18627885956
Fax
0573-85285100
Email
isenchem@163.com
Country
China
ProdList
9413
Advantage
66
Hunan Hui Bai Shi Biotechnology Co., Ltd.
Tel
0731-85526065 13308475853
Email
ivy@hnhbsj.com
Country
China
ProdList
4552
Advantage
62
S.Z. PhyStandard Bio-Tech. Co., Ltd.
Tel
0755-83725681-603
Fax
+86 755 28094224
Country
China
ProdList
4496
Advantage
50
Hefei Topway Biotechnology Co.,Ltd
Tel
0551-65326752 14755135869
Fax
0086-551-65326751
Email
xxhasym@163.com
Country
China
ProdList
70
Advantage
60
Guangzhou Isun Pharmaceutical Co., Ltd
Tel
020-39119399 18927568969
Fax
020-39119999
Email
isunpharm@qq.com
Country
China
ProdList
4428
Advantage
55
Nanjing Sunlida Biological Technology Co., Ltd.
Tel
025-57798810
Fax
025-57019371
Email
sales@sunlidabio.com
Country
China
ProdList
3239
Advantage
55
Shanghai Run-Biotech Co., Ltd.
Tel
021-57171705 13817537615
Fax
QQ3095748324
Email
sales@run-biotech.com
Country
China
ProdList
2427
Advantage
58
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View Lastest Price from Acotiamide hydrochloride trihydrate manufacturers

Hebei Yanxi Chemical Co., Ltd.
Product
Acotiamide hydrochloride trihydrate 773092-05-0
Price
US $0.00/kg
Min. Order
1kg
Purity
99% HPLC
Supply Ability
500kg/week
Release date
2023-09-15
Hebei Kingfiner Technology Development Co.Ltd
Product
Acotiamide hydrochloride trihydrate 773092-05-0
Price
US $0.00-0.00/kg
Min. Order
1kg
Purity
99%
Supply Ability
500000kg
Release date
2024-06-12
Wuhan Boyuan Import & Export Co., LTD
Product
Bulk AcotiaMide hydrochloride hydrate CAS NO.773092-05-0 773092-05-0
Price
US $1.00/G
Min. Order
100G
Purity
99.9%
Supply Ability
50000 tons
Release date
2018-11-06

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