product name Candesartan Cilexetil
Description: Candesartan Cilexetil (also known as TCV-116) is an angiotensin II receptor antagonist with IC50 of 0.26 nM, it is used in the treatment of hypertension. Candesartan Celexetil Ester is an ester analog of the angiotensin II antagonist Candesartan (sc-217825). Antagonism of this receptor prevents the binding of angiotensin II, a potent vasoconstrictor. This has the overall effect of vasodilation and an increased capillary blood volume. Candesartan Celexetil Ester is an inhibitor of AT1.
References: Am J Health Syst Pharm. 2000 Apr 15;57(8):739-46; Toxicology. 2012 Jan 27;291(1-3):139-45.
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)
Solubility (In vivo)
Synonyms
TCV-116
other peoduct :
| 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. Kinase Assay: Cell Assay: |
|---|---|
| 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 | |
| Formulation & Dosage | |
| References | Am J Health Syst Pharm. 2000 Apr 15;57(8):739-46; Toxicology. 2012 Jan 27;291(1-3):139-45. |
