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    Candesartan Cilexetil (CV 11974)
    Candesartan Cilexetil (CV 11974)

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    This product is for research use only, not for human use. We do not sell to patients.
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    InvivoChem Cat #: V1784
    CAS #: 145040-37-5Purity ≥98%

    Description: Candesartan Cilexetil (formerly TCV-116; CV11974; CV-11974; Atacand), an ester prodrug of Candesartan, is an antihypertensive drug acting as an AT II/angiotensin II receptor antagonist with anti-hypertensive effects. It inhibits AT II with an IC50 of 0.26 nM. Candesartan is an approved medication primarily used for the treatment of hypertension. It is marketed as the cilexetil ester, which is known as candesartan cilexetil. Candesartan cilexetil is metabolized completely by esterase in the intestinal wall during absorption to the active candesartan moiety. The use of a prodrug form increases the bioavailability of candesartan.

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

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    Molecular Weight (MW)610.66 
    FormulaC33H34N6O6 
    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

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


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    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. 


    These protocols are for reference only. InvivoChem does not independently validate these methods.

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