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Candesartan

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Candesartan Basic information

Product Name:
Candesartan
Synonyms:
  • 1-((2'-(1H-Tetrazol-5-yl)-[1,1'-biphenyl]-4-yl)Methyl)-2-ethoxy-1H-benzo[d]iMidazole-7-carboxylic acid
  • 2-ethoxy-3-[[4-[2-(1h-tetrazol-5-yl)phenyl]phenyl]methyl]-3h-benzoimidazole-4-carboxylic acid
  • 3-[[2'-(1H-Tetrazol-5-yl)biphenyl-4-yl]Methyl]-2-ethoxy-3H-benziMidazole-4- carboxylic Acid
  • Candesartan M1
  • 2-ETHOXY1-2(1H-TETRAZOL-5YL)1,1-BIPHENYL)-4-YL)-4-YL)METHYL)1H-BENZIMIDAZOLE-7-CARBOXYLIC ACID
  • Candesartan Cilexetil EP IMpurity G
  • 1-((2'-(1H-Tetrazol-5-yl)-[1,1'-biphenyl]-4-yl)methyl)-2-ethoxy-1H-benzo[d]imidazole-7-carboxylic
  • 1H-Benzimidazole-7-carboxylic acid, 2-ethoxy-1-[[2'-(2H-tetrazol-5-yl)[1,1'-biphenyl]-4-yl]methyl]-
CAS:
139481-59-7
MF:
C24H20N6O3
MW:
440.45
EINECS:
604-138-8
Product Categories:
  • Isotope
  • Pharmaceutical raw material
  • Bases & Related Reagents
  • Intermediates & Fine Chemicals
  • Aromatics
  • Heterocycles
  • Active Pharmaceutical Ingredients
  • Candesartan Cilexetil
  • API intermediates
  • Nucleotides
  • Pharmaceuticals
  • Candesartan Cilexatil
Mol File:
139481-59-7.mol
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Candesartan Chemical Properties

Melting point:
183-185°C
Boiling point:
754.8±70.0 °C(Predicted)
Density 
1.41±0.1 g/cm3(Predicted)
RTECS 
DD6671000
storage temp. 
Inert atmosphere,Store in freezer, under -20°C
solubility 
Soluble in DMSO (up to 40 mg/ml)
pka
2.06±0.10(Predicted)
form 
solid
color 
White
Water Solubility 
Soluble in ethyl acetate, methanol, water (<1 mg/ml at 25°C), DMSO (88 mg/ml at 25°C), and ethanol (1 mg/ml at 25°C).
Stability:
Stable for 1 year from date of purchase as supplied. Solutions in DMSO may be stored at -20°C for up to 2 months.
CAS DataBase Reference
139481-59-7(CAS DataBase Reference)
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Safety Information

Hazard Codes 
Xn
Risk Statements 
20/21/22-36/37/38
Safety Statements 
26-36-60-36/37-9
HS Code 
29419000
Hazardous Substances Data
139481-59-7(Hazardous Substances Data)
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Candesartan Usage And Synthesis

Description

Candesartan (CAS 139481-59-7) is an angiotensin II receptor I (AT1) antagonist, IC50s=1.12 and 2.86 nM for bovine adrenal cortex and rabbit aorta respectively.1?Selectively inhibits angiotensin II-induced contraction of rabbit aortic strips with no effect on contraction induced by other agents such as norepinephrine, KCl, serotonin, PGF2αor endothelin. Prevents astrocyte and microglial activation and neuroinflammation and improves hippocampal neurogenesis.2?Attenuates angiogenesis in hepatocellular carcinoma.3?Clinically useful antihypertensive agent. Ameliorates brain inflammation associated with Alzheimer’s disease.4?Active?in vivo?and orally active.

Chemical Properties

Crystalline Solid

Uses

An angiotensin II type-1 receptor antagonist. Used in treatment of congestive heart failure. Antihypertensive

Uses

antihypertensive, angiotensin II inhibitor

Uses

Candesartan is a selective AT1 (angiotensin II receptor 1) antagonist. Antagonism of angiotensin receptors inhibits vasoconstriction and the production of aldosterone, leading to a decrease in water and sodium concentration in blood plasma. Exhibits antihypertensive effects in animal models. Used in treatment of congestive heart failure, as antihypertensive. Candesartan does not affect cell viability or proliferation but increases the expression of VEGF and interleukin-8 in the cultured medium of KU-19-19 cells. Candesartan (0.1 nM) could reduce the maximal contractile response to angiostensin II by approximately 50%.

Definition

ChEBI: A benzimidazolecarboxylic acid that is 1H-benzimidazole-7-carboxylic acid substituted by an ethoxy group at position 2 and a ({2'-(1H-tetrazol-5-yl)[1,1'-biphenyl]-4-yl}methyl) group at position 1. It is a angiotensin eceptor antagonist used for the treatment of hypertension.

brand name

Atacand (AstraZeneca).

General Description

Candesartan, (+)-1-[[(cyclohexyloxy)carbonyl]-oxy]ethyl 2- ethoxy-1-[[2'-(1H-tetrazol-5-yl)[1,1'-biphenyl]-4-yl]methyl]-1H-benzimidazole-7-carboxylate(Atacand), like losartan, possesses the acidic tetrazole system,which most likely plays a role in binding to the angiotensin IIreceptor similarly to the acidic groups of angiotensin II. Also,the imidazole system has been replaced with a benzimidazolepossessing an ester at position. This ester must be hydrolyzedto the free acid. Fortunately, this conversion takesplace fairly easily because of the carbonate in the ester sidechain. This facilitates hydrolysis of the ester so much thatconversion to the free acid takes place during absorption fromthe gastrointestinal tract.

storage

Store at RT

References

1) Shibouta?et al.?(1993),?Pharmacological profile of a highly potent and long-acting angiotension II receptor antagonist, 2-ethoxy-1-[[2’-(1H-tetrazol-5-yl)biphenyl-4-yl]methyl]-1H-benzimidazol-7-carboxylic acid (CV-11974), and its prodrug, (+/-)-1-(cyclohexyloxycarbonyloxy)-ethyl 2-ethoxy-1-[[2’-(1H-tetrazol-5-yl)biphenyl-4-yl]methyl]-1H-benzimidazole-7-carboxylate (TCV-116); J. Pharmacol. Exp. Therap.,?266?114 2) Bhat?et al. (2017),?Angiotensin receptor Blockade by Inhibiting Glial Activation Promotes Hippocampal Neurogenesis Via Activation of Wnt/B-Catenin signaling in hypertension; Mol. Neurobiol.,?55 5282 3) Fan?et al.?(2016),?Candesartan attenuates angiogenesis in hepatocellular carcinoma via downregulating AT1R/VEGF pathway; Biomed. Pharmacother.,?83?704 4) Torika?et al.?(2018),?Candesartan ameliorates brain inflammation associated with Alzheimer’s disease; CNS Neurosci. Ther.?24?231

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