Candesartan Cilexetil (CV 11974)

Alias: CV-11974; TCV-116; CV 11974;TCV 116;CV11974; TCV116
Cat No.:V1784 Purity: ≥98%
Candesartan Cilexetil (formerly TCV-116;CV11974; CV-11974; Atacand), an ester prodrug ofCandesartan,is an antihypertensive drug acting as an AT II/angiotensin II receptor antagonistwith anti-hypertensive effects.
Candesartan Cilexetil (CV 11974) Chemical Structure CAS No.: 145040-37-5
Product category: RAAS
This product is for research use only, not for human use. We do not sell to patients.
Size Price Stock Qty
500mg
1g
2g
5g
50g
Other Sizes

Other Forms of Candesartan Cilexetil (CV 11974):

  • Candesartan (CV 11974)
  • Candesartan D4 (CV-11974 D4)
Official Supplier of:
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Purity & Quality Control Documentation

Purity: ≥98%

Product 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.

Biological Activity I Assay Protocols (From Reference)
ln 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.

ln 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 Protocol
1 mg/kg, p.o.
Rats
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.
Physicochemical Properties
Molecular Formula
C33H34N6O6
Molecular Weight
610.66
CAS #
145040-37-5
Related CAS #
Candesartan;139481-59-7;Candesartan-d4;1346604-70-3
SMILES
O(C(=O)OC([H])(C([H])([H])[H])OC(C1C([H])=C([H])C([H])=C2C=1N(C(=N2)OC([H])([H])C([H])([H])[H])C([H])([H])C1C([H])=C([H])C(C2=C([H])C([H])=C([H])C([H])=C2C2N=NN([H])N=2)=C([H])C=1[H])=O)C1([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C1([H])[H]
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)
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
Synonyms
CV-11974; TCV-116; CV 11974;TCV 116;CV11974; TCV116
Storage

Powder      -20°C    3 years

                     4°C     2 years

In solvent   -80°C    6 months

                  -20°C    1 month

Shipping Condition
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
Solubility Data
Solubility (In Vitro)
DMSO:122 mg/mL (199.8 mM)
Water:<1 mg/mL
Ethanol:4 mg/mL (6.6 mM)
Solubility (In Vivo)
Solubility in Formulation 1: ≥ 2.5 mg/mL (4.09 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL.
Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution.

Solubility in Formulation 2: ≥ 2.5 mg/mL (4.09 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly.

 (Please use freshly prepared in vivo formulations for optimal results.)
Preparing Stock Solutions 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

*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.

Calculator

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An example of molarity calculation using the molarity calculator is shown below:
What is the mass of compound required to make a 10 mM stock solution in 5 ml of DMSO given that the molecular weight of the compound is 350.26 g/mol?
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  • The answer of 17.513 mg appears in the Mass box. In a similar way, you may calculate the volume and concentration.

Dilution Calculator allows you to calculate how to dilute a stock solution of known concentrations. For example, you may Enter C1, C2 & V2 to calculate V1, as detailed below:

What volume of a given 10 mM stock solution is required to make 25 ml of a 25 μM solution?
Using the equation C1V1 = C2V2, where C1=10 mM, C2=25 μM, V2=25 ml and V1 is the unknown:
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g/mol

Molecular Weight Calculator allows you to calculate the molar mass and elemental composition of a compound, as detailed below:

Note: Chemical formula is case sensitive: C12H18N3O4  c12h18n3o4
Instructions to calculate molar mass (molecular weight) of a chemical compound:
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Definitions of molecular mass, molecular weight, molar mass and molar weight:
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In vivo Formulation Calculator (Clear solution)
Step 1: Enter information below (Recommended: An additional animal to make allowance for loss during the experiment)
Step 2: Enter in vivo formulation (This is only a calculator, not the exact formulation for a specific product. Please contact us first if there is no in vivo formulation in the solubility section.)
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Calculation results

Working concentration mg/mL;

Method for preparing DMSO stock solution mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.

Method for preparing in vivo formulation:Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O,mix and clarify.

(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
             (2) Be sure to add the solvent(s) in order.

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