[CAS NO. 145040-37-5] Candesartan Cilexetil

Name: Candesartan Cilexetil
Brand: Arctom Scientific
SKU: SLK-S2037

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PRODUCTS SPECIFICATIONS [145040-37-5]

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Catalog

SLK-S2037

Brand

Selleck

CAS

145040-37-5

DESCRIPTION [145040-37-5]

Overview

MDL	MFCD00871371
Molecular Weight	610.66
Molecular Formula	C33H34N6O6
SMILES	C(N1C=2C(N=C1OCC)=CC=CC2C(OC(OC(OC3CCCCC3)=O)C)=O)C4=CC=C(C=C4)C5=C(C=CC=C5)C=6NN=NN6

For research use only.

Storage

3 years,-20°C,powder
1 years,-80°C,in solvent

Shipping

Room temperature shipping(Stability testing shows this product can be shipped without any cooling measures.)

Preparing Stock Solutions

Concentration Volume Mass	1 mg	5 mg	10 mg
1 mM	1.6376 mL	8.1879 mL	16.3757 mL
5 mM	0.3275 mL	1.6376 mL	3.2751 mL
10 mM	0.1638 mL	0.8188 mL	1.6376 mL
50 mM	0.0328 mL	0.1638 mL	0.3275 mL

Description

Candesartan Cilexetil (TCV-116) is an antagonist with of 0.26 nM, used in the treatment of hypertension.

Targets

Ang II receptor ^[1]

0.26 nM

In vitro

Candesartan blocks the effects of angiotensin II at the angiotensin II type 1 (AT1) receptor. Candesartan cilexetil is a prodrug that is activated to candesartan by ester hydrolysis during gastrointestinal absorption.

In vivo

Candesartan improves the functional markers in a dose-dependent manner and also upregulates Ang (1-7), ACE2 and mas1 in the myocardium of DCM rats. Candesartan reduces various ER stress and apoptosis markers and the number apoptotic cells in the Candesartan treated rats. Candesartan cilexetil shows angiotensin-II blocking action in a dose-dependent manner in rats with dilated cardiomyopathy. Candesartan cilexetil reduces the left ventricular end-diastolic pressure and heart weight/body weight ratio, the area of myocardial fibrosis and expressions of transforming growth factor-beta1 and collagen-III mRNA. Candesartan cilexetil (1 mg/kg, p.o.) and enalapril (10 mg/kg, p.o.) reduces blood pressure to the same extent 5 hours after administration on the 1st and the 7th day. Candesartan cilexetil significantly increases renal blood flow without any changes in the cardiac index. TCV-116 and enalapril also tends to increase splanchnic blood flow following the 1st dose but not the 7th dose. Candesartan cilexetil is absorbed from the small intestine and hydrolyzed completely to the pharmacologically active metabolite M-I during absorption process.

References

[1] See S, et al. Am J Health Syst Pharm,?000,?7(8), 739-746.
[2] Arumugam S, et al. Toxicology,?012, 291(1-3), 139-145.
[3] Shirai K, et al. Mol Cell Biochem,?005, 269(1-2), 137-142.
[4] Kanagawa R, et al. Jpn J Pharmacol,?997, 73(3), 185-190.
[5] Kondo T, et al. Arzneimittelforschung,?996, 46(6), 594-600.

Synonyms

1H-Benzimidazole-7-carboxylic acid, 2-ethoxy-1-[[2′-(2H-tetrazol-5-yl)[1,1′-biphenyl]-4-yl]methyl]-, 1-[[(cyclohexyloxy)carbonyl]oxy]ethyl ester

1H-Benzimidazole-7-carboxylic acid, 2-ethoxy-1-[[2′-(1H-tetrazol-5-yl)[1,1′-biphenyl]-4-yl]methyl]-, 1-[[(cyclohexyloxy)carbonyl]oxy]ethyl ester, (±)-

1H-Benzimidazole-7-carboxylic acid, 2-ethoxy-1-[[2′-(1H-tetrazol-5-yl)[1,1′-biphenyl]-4-yl]methyl]-, 1-[[(cyclohexyloxy)carbonyl]oxy]ethyl ester

TCV 116

(±)-1-Hydroxyethyl 2-ethoxy-1-[p-(o-1H-tetrazol-5-ylphenyl)l]-7-benzimidazolecarboxylate, cyclohexyl carbonate (ester)

Candesartan cilexetil

Atacand

TCY 116

Blopress

2-Ethoxy-1-[(2′-(1H-tetrazol-5-yl)-1,1′-biphenyl-4-yl)methyl]-7-benzimidazolecarboxylic acid 1-(cyclohexyloxycarbonyloxy)ethyl ester

1-[[(Cyclohexyloxy)carbonyl]oxy]ethyl 2-ethoxy-1-[[2′-(1H-tetrazol-5-yl)biphenyl-4-yl]methyl]benzimidazole-7-carboxylate

1-Cyclohexyloxycarbonyloxyethyl 2-ethoxy-3-[[4-[2-(2H-tetrazol-5-yl)phenyl]phenyl]methyl]benzimidazole-4-carboxylate

1-[[(Cyclohexyloxy)carbonyl]oxy]ethyl 2-ethoxy-1-([4-[2-(1H-1,2,3,4-tetrazol-5-yl)phenyl]phenyl]methyl)-1H-1,3-benzodiazole-7-carboxylate