Candesartan Cilexetil(CV 11974)

Molecular Weight (MW)	610.66
Formula	C33H34N6O6
CAS No.	145040-37-5
Storage	-20℃ for 3 years in powder form
-80℃ for 2 years in solvent
Solubility (In vitro)	DMSO: 122 mg/mL (199.8 mM)
Water: <1 mg/mL
Ethanol: 4 mg/mL (6.6 mM)
Other info	Chemical Name: 1-(((cyclohexyloxy)carbonyl)oxy)ethyl 1-((2'-(1H-tetrazol-5-yl)-[1,1'-biphenyl]-4-yl)methyl)-2-ethoxy-1H-benzo[d]imidazole-7-carboxylate InChi Key: GHOSNRCGJFBJIB-UHFFFAOYSA-N InChi Code: InChI=1S/C33H34N6O6/c1-3-42-32-34-28-15-9-14-27(31(40)43-21(2)44-33(41)45-24-10-5-4-6-11-24)29(28)39(32)20-22-16-18-23(19-17-22)25-12-7-8-13-26(25)30-35-37-38-36-30/h7-9,12-19,21,24H,3-6,10-11,20H2,1-2H3,(H,35,36,37,38) SMILES Code: O=C(OC(C)OC(C1=CC=CC2=C1N(CC3=CC=C(C4=C(C5=NN=NN5)C=CC=C4)C=C3)C(OCC)=N2)=O)OC6CCCCC6
Synonyms	CV-11974; TCV-116; CV 11974; TCV 116; CV11974; TCV116

Molecular Weight (MW)

610.66

Formula

C33H34N6O6

CAS No.

145040-37-5

Storage

-20℃ for 3 years in powder form

-80℃ for 2 years in solvent

Solubility (In vitro)

DMSO: 122 mg/mL (199.8 mM)

Water: <1 mg/mL

Ethanol: 4 mg/mL (6.6 mM)

Other info

Chemical Name: 1-(((cyclohexyloxy)carbonyl)oxy)ethyl 1-((2'-(1H-tetrazol-5-yl)-[1,1'-biphenyl]-4-yl)methyl)-2-ethoxy-1H-benzo[d]imidazole-7-carboxylate

InChi Key: GHOSNRCGJFBJIB-UHFFFAOYSA-N

InChi Code: InChI=1S/C33H34N6O6/c1-3-42-32-34-28-15-9-14-27(31(40)43-21(2)44-33(41)45-24-10-5-4-6-11-24)29(28)39(32)20-22-16-18-23(19-17-22)25-12-7-8-13-26(25)30-35-37-38-36-30/h7-9,12-19,21,24H,3-6,10-11,20H2,1-2H3,(H,35,36,37,38)

SMILES Code: O=C(OC(C)OC(C1=CC=CC2=C1N(CC3=CC=C(C4=C(C5=NN=NN5)C=CC=C4)C=C3)C(OCC)=N2)=O)OC6CCCCC6

Synonyms

CV-11974; TCV-116; CV 11974; TCV 116; CV11974; TCV116

In Vitro	In vitro activity: 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.
Animal model	Rats
Formulation & Dosage	1 mg/kg, p.o.
References	Am J Health Syst Pharm. 2000 Apr 15;57(8):739-46; Toxicology. 2012 Jan 27;291(1-3):139-45.

In Vitro

In vitro activity: 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.

Animal model

Rats

Formulation & Dosage

1 mg/kg, p.o.

References

Am J Health Syst Pharm. 2000 Apr 15;57(8):739-46; Toxicology. 2012 Jan 27;291(1-3):139-45.

CAS NO:	145040-37-5
规格:	≥98%

包装	价格(元)
500mg	电议
1g	电议
2g	电议
5g	电议
50g	电议