Candesartan Cilexetil - Moligand™, 10mM in DMSO , Type-1 angiotensin II receptor antagonist, CAS No.145040-37-5, Type-1 angiotensin II receptor antagonist

CAS: 145040-37-5 Cat. No.: C408897 Molecular Weight: 610.66 EC Number: 627-030-2

GRADE & PURITY Moligand™, 10mM in DMSO

Synonyms

TCV-116 | 2-​ethoxy-​1-​[[2'-​(2H-​tetrazol-​5-​yl)​[1,​1'-​biphenyl]​-​4-​yl]​methyl]​-1H-​benzimidazole-​7-​carboxylic acid-1-​[[(cyclohexyloxy)​carbonyl]​oxy]​ethyl ester

Storage

Store at -80°C

Shipped In

Dry ice packs + Cold packs

Overview

Information

Candesartan Cilexetil Candesartan Cilexetil (TCV-116) is an angiotensin II receptor antagonist with IC50 of 0.26 nM, used in the treatment of hypertension.
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.
Cell Data

cell lines：

Concentrations：

Incubation Time：

Powder Purity:≥99%

Specifications

Synonyms

TCV-116 | 2-​ethoxy-​1-​[[2'-​(2H-​tetrazol-​5-​yl)​[1, ​1'-​biphenyl]​-​4-​yl]​methyl]​-1H-​benzimidazole-​7-​carboxylic acid-1-​[[(cyclohexyloxy)​carbonyl]​oxy]​ethyl ester

Specifications & Purity

Moligand™, 10mM in DMSO

Biochemical and Physiological Mechanisms

Candesartan Cilexetil (TCV-116) is an angiotensin II receptor antagonist with IC50 of 0.26 nM, used in the treatment of hypertension.

Storage

Store at -80°C

Shipped In

Dry ice packs + Cold packs

This product requires cold chain shipping. Ground and other economy services are not available.

Grade

Moligand™

Action Type

ANTAGONIST

Mechanism of action

Type-1 angiotensin II receptor antagonist

Product Properties

• ALogP: 7

Names and Identifiers

• Isomeric SMILES: CCOC1=NC2=CC=CC(=C2N1CC3=CC=C(C=C3)C4=CC=CC=C4C5=NNN=N5)C(=O)OC(C)OC(=O)OC6CCCCC6
• WGK Germany: 3
• RTECS: DD6672500
• Molecular Weight: 610.66
• Reaxy-Rn: 6362591
• Reaxys-RN_link_address: https://www.reaxys.com/reaxys/secured/hopinto.do?context=S&query=IDE.XRN=6362591&ln=

Associated Targets(Human)

SLCO1B1 Tchem Solute carrier organic anion transporter family member 1B1 (2 Activities)

Discover Target: SLCO1B1

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

Chemical and Physical Properties

• Melt Point(°C): 159 °C

References

1. Zhang Lei, Zhang Shi-tao, Zhang Xiao-ping, Sun Jing, Wang Yong-sen, Liu Yue-long, Xue Miao-miao, Wang Zhi, Xing Shu, Ma Jun-feng, Li Wan-nan, Fu Xue-qi.  (2013)  Effect of Candesartan cilexetil as a sensitive and effective inhibitor of SHP-1 on insulin signaling pathway.  CHEMICAL RESEARCH IN CHINESE UNIVERSITIES,  29  (4): (730-734).  [PMID:] [10.1007/s40242-013-2505-0]

2. Qi Liang, Xiaoying Fu, Jianfeng Zhang, Jiaxue Hao, Gangjun Feng, Jing Wang, Qian Li, Faizan Ahmad, Xinfeng Zhao.  (2020)  Immobilized angiotensin II type I receptor: A powerful method of high throughput screening for antihypertensive compound identification through binding interaction analysis.  JOURNAL OF CHROMATOGRAPHY A,      [PMID:32156458] [10.1016/j.chroma.2020.461003]