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Azilsartan Medoxomil

Azilsartan Medoxomil Structure
Azilsartan Medoxomil structure
CAS No.
863031-21-4
Chemical Name:
Azilsartan Medoxomil
Synonyms
TAK 491;Azilsartan MedoxiMil;CS-306;Azizartan ester;Azilsaran medoxomil;Azilsartan medoxomil;Azilsartan MedoxoMil(TAK 491);Azilsartan Kamedoxomil Form I;Azilsartan Medoxomil USP/EP/BP;Azilsartan Acid Medoxomil Ester
CBNumber:
CB32516566
Molecular Formula:
C30H24N4O8
Molecular Weight:
568.53
MDL Number:
MFCD19443688
MOL File:
863031-21-4.mol
MSDS File:
SDS
Last updated:2023-07-05 17:39:42
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Azilsartan Medoxomil Properties

Melting point 160-161oC
Density 1.45
storage temp. Refrigerator
solubility DMSO (Slightly), Methanol (Slightly, Heated, Sonicated)
pka 6.99±0.20(Predicted)
form Solid
color White to Light Beige
FDA UNII LL0G25K7I2
ATC code C09CA09

SAFETY

Risk and Safety Statements

Symbol(GHS)  GHS hazard pictograms
GHS07
Signal word  Warning
Hazard statements  H302-H315-H319-H335
Precautionary statements  P261-P305+P351+P338
NFPA 704
0
2 0

Azilsartan Medoxomil price More Price(27)

Manufacturer Product number Product description CAS number Packaging Price Updated Buy
Cayman Chemical 23805 Azilsartan Medoxomil ≥98% 863031-21-4 1mg $44 2024-03-01 Buy
Cayman Chemical 23805 Azilsartan Medoxomil ≥98% 863031-21-4 5mg $193 2024-03-01 Buy
Cayman Chemical 23805 Azilsartan Medoxomil ≥98% 863031-21-4 10mg $321 2024-03-01 Buy
Cayman Chemical 23805 Azilsartan Medoxomil ≥98% 863031-21-4 25mg $692 2024-03-01 Buy
TRC A926910 AzilsartanMedoxomil 863031-21-4 100mg $40 2021-12-16 Buy
Product number Packaging Price Buy
23805 1mg $44 Buy
23805 5mg $193 Buy
23805 10mg $321 Buy
23805 25mg $692 Buy
A926910 100mg $40 Buy

Azilsartan Medoxomil Chemical Properties,Uses,Production

Description

Azilsartan medoxomil (Edarbi), an angiotensin II receptor antagonist, was approved by the U.S. FDA in February 2011 for the treatment of hypertension in adults. The discovery of azilsartan was the result of a medicinal chemistry effort to identify an ARB with a different carboxylic acid isostere than the ones found in the marketed ARBs. Several of the marketed ARBs use a tetrazole group as a carboxylic acid isostere. The medicinal chemistry approach that led to azilsartan involved the replacement of this commonly used tetrazole with a 5-oxo-1,2,4-oxadiazole group. Azilsartan can be synthesized by Suzuki coupling of p-tolyl boronic acid to 2-bromobenzonitrile, followed by bromination of the methyl group. The bromide is displaced to introduce a protected 2-ethoxy-1H-benzo[d] imidazole-7-carboxylate. The cyano group is converted to a hydroxylamidine, followed by reaction with an alkyl-chloroformate and intramolecular cyclization to form the 5-oxo-1,2,4-oxadiazole ring. The acid is then deprotected and converted to a prodrug. The parent, azilsartan has been extensively characterized in vitro and compared with other marketed AT1 antagonists olmesartan, valsartan, telmisartan, irbesartan, and candesartan. Azilsartan was found to be a potent (IC50=2.6 nM), selective, inverse agonist of the AT1 receptor. From washout experiments, azilsartan was found have slow dissociation from the receptor and thus is characterized as an insurmountable antagonist.

Description

Azilsartan medoxomil is a prodrug form of azilsartan , a potent and selective angiotensin II receptor 1 (AT1) antagonist. Azilsartan medoxomil (0.1-10 mg/kg) reduces blood pressure and decreases plasminogen activator inhibitor 1 (PAI-1) levels in the plasma, left ventricle, and aortic wall in mice in a dose-dependent manner. It also inhibits the pressor response induced by angiotensin II in normotensive rats (ID50 = 0.12 mg/kg) and reduces blood pressure and improves glucose infusion, a marker of insulin sensitivity, in spontaneously hypertensive rats. Azilsartan medoxomil also has more potent antiproteinuric effects in Wistar fatty rats than olmesartan medoxomil . Formulations containing azilsartan medoxomil have been used in the treatment of hypertension.

Originator

Takeda (United States)

Uses

Azilsartan medoxomil is a long-acting angiotensin II receptor blocker (ARB) that is used to lower hypertension. When Azilsartan medoxomil enters the gastrointestinal tract, it is rapidly converted to its active form, Azilsartan (A926900).

Definition

ChEBI: A carboxylic ester obtained by formal condensation of the carboxy group of azilsartan with the hydroxy group of 4-(hydroxymethyl)-5-methyl-1,3-dioxol-2-one. A prodrug for azilsartan, it is used for treatment of hypertension.

brand name

Edarbi

Azilsartan Medoxomil synthesis

91526-18-0
147403-03-0
863031-21-4
Synthesis of Azilsartan Medoxomil from 4-(Hydroxymethyl)-5-methyl-1,3-dioxol-2-one and Azilsartan

Azilsartan Medoxomil Preparation Products And Raw materials

Raw materials

Preparation Products

Azilsartan Medoxomil Suppliers

Global( 249)Suppliers
Supplier Tel Email Country ProdList Advantage
Capot Chemical Co.,Ltd. 		571-85586718 +8613336195806 sales@capotchem.com China 29797 60
Henan Tianfu Chemical Co.,Ltd. 		+86-0371-55170693 +86-19937530512 info@tianfuchem.com China 21695 55
career henan chemical co 		+86-0371-86658258 sales@coreychem.com China 29914 58
Hubei xin bonus chemical co. LTD 		86-13657291602 linda@hubeijusheng.com CHINA 22968 58
BOC Sciences 		+1-631-485-4226 inquiry@bocsci.com United States 19553 58
Chongqing Chemdad Co., Ltd 		+86-023-61398051 +8613650506873 sales@chemdad.com China 39916 58
Alchem Pharmtech,Inc. 		8485655694 sales@alchempharmtech.com United States 63711 58
CONIER CHEM AND PHARMA LIMITED 		+8618523575427 sales@conier.com China 47465 58
Fuxin Pharmaceutical 		+86-021-021-50872116 +8613122107989 contact@fuxinpharm.com China 10297 58
Neostar United (Changzhou) Industrial Co., Ltd. 		+86-519-519-85557386 marketing1@neostarunited.com China 8349 58
Supplier Advantage
Capot Chemical Co.,Ltd. 		60
Henan Tianfu Chemical Co.,Ltd. 		55
career henan chemical co 		58
Hubei xin bonus chemical co. LTD 		58
BOC Sciences 		58
Chongqing Chemdad Co., Ltd 		58
Alchem Pharmtech,Inc. 		58
CONIER CHEM AND PHARMA LIMITED 		58
Fuxin Pharmaceutical 		58
Neostar United (Changzhou) Industrial Co., Ltd. 		58

View Lastest Price from Azilsartan Medoxomil manufacturers

Image Update time Product Price Min. Order Purity Supply Ability Manufacturer
Azilsartan Medoxomil pictures 2024-01-08 Azilsartan Medoxomil
863031-21-4
 US $19.00-12.00 / kg 1kg 99.50% 20tons Wuhan Boyuan Import & Export Co., LTD
Azilsartan Medoxomil pictures 2022-02-23 Azilsartan Medoxomil
863031-21-4
 US $9.90-7.70 / g 10g 99.99%HPLC.USP42——Powder、Oil、Pills、Capsules、Tablets，Customiz 1000kgs Shanghai Biolang Biotechnology Co., Ltd.
Azilsartan Medoxomil pictures 2021-07-13 Azilsartan Medoxomil
863031-21-4
 US $15.00-10.00 / KG 1KG 99%+ HPLC Monthly supply of 1 ton Zhuozhou Wenxi import and Export Co., Ltd
  • Azilsartan Medoxomil pictures
  • Azilsartan Medoxomil
    863031-21-4
  • US $9.90-7.70 / g
  • 99.99%HPLC.USP42——Powder、Oil、Pills、Capsules、Tablets，Customiz
  • Shanghai Biolang Biotechnology Co., Ltd.
  • Azilsartan Medoxomil pictures
  • Azilsartan Medoxomil
    863031-21-4
  • US $15.00-10.00 / KG
  • 99%+ HPLC
  • Zhuozhou Wenxi import and Export Co., Ltd

Azilsartan Medoxomil Spectrum

Azilsartan Medoxomil(863031-21-4)1HNMR

863031-21-4(Azilsartan Medoxomil)Related Search:

TAK 599 methyl ((1S,2R,3S,4R)-2,3-dihydroxy-4-((2-(3-((trifluoromethyl)thio)phenyl)pyrazolo[1,5-a]pyrimidin-7-yl)amino)cyclopentyl)sulfamate 4-(Hydroxymethyl)-5-methyl-1,3-dioxol-2-one 2-[Bis[(1,1-diMethylethoxy)carbonyl]aMino]-3-nitrobenzoic Acid Methyl Ester BENZOIC ACID, 2-[[(2'-CYANO[1,1'-BIPHENYL]-4-YL)METHYL]AMINO]-3-NITRO-METHYL ESTER
Methyl 3-aMino-2-((2'-carbaMoylbiphenyl-4-yl)MethylaMino)benzoate Ethyl-3-Amino-2-[(2'-Cyanoiphenyl-4-yl) Methyl]-Amino Benzoate (Z)-2-ethoxy-3-((2'-(N'-hydroxycarbaMiMidoyl)biphenyl-4-yl)Methyl)-3H-benzo[d]iMidazole-4-carboxylic acid (Z)-Methyl 3-((2'-(N'-hydroxycarbaMiMidoyl)biphenyl-4-yl)Methyl)-2-oxo-2,3-dihydro-1H-benzo[d]iMidazole-4-carboxylate Azilsartan iMpurity I
Methyl 2-oxo-3-((2'-(5-oxo-4,5-dihydro-1,2,4-oxadiazol-3-yl)biphenyl-4-yl)Methyl)-2,3-dihydro-1H-benzo[d]iMidazole-4-carboxylate 1H-BenziMidazole-7-carboxylic acid, 1-[[2'-(2,5-dihydro-5-oxo-1,2,4-oxadiazol-3-yl)[1,1'-biphenyl]-4-yl]Methyl] -2-ethoxy-, Methyl ester Azilsartan kaMedoxoMil (Z)-Methyl 2-ethoxy-3-((2'-(N'-hydroxycarbaMiMidoyl)biphenyl-4-yl)Methyl)-3H-benzo[d] iMidazole-4-carboxylate Azilsartan
Zafirlukast Pitavastatin calcium Cetirizine dihydrochloride

1of4

1H-BenziMidazole-7-carboxylic acid, 1-[[2'-(2,5-dihydro-5-oxo-1,2,4-oxadiazol-3-yl)[1,1'-biphenyl]-4-yl]Methyl]-2-ethoxy-, (5-Methyl-2-oxo-1,3-dioxol-4-yl)Methyl ester Azilsaran medoxomil (5-methyl-2-oxo-1,3-dioxol-4-yl)methyl 2-ethoxy-3-[[4-[2-(5-oxo-4H-1,2,4-+oxadiazol-3-yl)phenyl]phenyl]methyl]benzimidazole-4-carboxylate 1-[[2'-(2,5-Dihydro-5-oxo-1,2,4-oxadiazol-3-yl)[1,1'-biphenyl]-4-yl]methyl]-2-ethoxy-1H-benzim 1-[[2'-(2,5-Dihydro-5-oxo-1,2,4-oxadiazol-3-yl)[1,1'-biphenyl]-4-yl]methyl]-2-ethoxy-1H-benzimidazole-7-carboxylic acid (5-methyl-2-oxo-1,3-dioxol-4-yl)methyl ester Azilsartan medoxomil Azilsartan MedoxoMil(TAK 491) (5-Methyl-2-oxo-1,3-dioxol-4-yl)Methyl 2-ethoxy-1-([2'-(5-oxo-4,5-dihydro-1,2,4-oxadiazol-3-yl)biphenyl-4-yl]Methyl)-1H-benziMidazole-7-carboxylate CS-306 azilsartan medoxomil 1-[[2'-(2,5-Dihydro-5-oxo-1,2,4-oxadiazol-3-yl)[1,1'-biphenyl]-4-yl]methyl]-2-ethoxy-1H-benzimidazole-7-carboxylic acid (5-methyl-2-oxo-1,3-dioxol-4-yl)methyl ester Azilsartan Acid Medoxomil Ester Azilsartan Kamedoxomil Form I Azilsartan Medoxomil USP/EP/BP (5-methyl-2-oxo-1,3-dioxol-4-yl)methyl2-ethoxy-1-((2'-(5-oxo-2,5-dihydro-1,2,4-oxadiazol-3-yl)-[1,1'-biphenyl]-4-yl)methyl)-1H-benzo[d]imidazole-7-carboxylate Azilsartan medoxomilQ: What is Azilsartan medoxomil Q: What is the CAS Number of Azilsartan medoxomil Q: What is the storage condition of Azilsartan medoxomil Q: What are the applications of Azilsartan medoxomil Azizartan ester Azilsartan MedoxiMil TAK 491 (5-Methyl-2-oxo-1,3-dioxol-4-yl)methyl 2-ethoxy-1-((2'-(5-oxo-4,5-dihydro-1,2,4-oxadiazol-3-yl)-[1,1'-biphenyl]-4-yl)methyl)-1H-benzo[d]imidazole-7-carboxylate (5-Methyl-2-oxo-1,3-dioxol-4-yl)methyl 2-ethoxy-1-((2'-(5-oxo-4,5-dihydro-1,2,4-oxadiazol-3-yl)-[1,1'-biphenyl]-4-yl)methyl)-1H-benzo[d]imidazole-7-carboxylate 863031-21-4 C30H24N4O8 Azilsartan Medoxomil Inhibitors