Candesartan Cilexetil [145040-37-5]

Cat# HY-17505-1ml

Size : 10mM/1mL

Brand : MedChemExpress

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Description

Candesartan Cilexetil (TCV-116) is an angiotensin II receptor inhibitor. Candesartan Cilexetil ameliorates the pulmonary fibrosis and has antiviral and skin wound healing effect. Candesartan Cilexetil can be used for the research of high blood pressure[1][2][3][4][5][6].

Cellular Effect
Cell Line Type Value Description References
16HBE14o- IC50
> 100 μM
Compound: 1; CDC, MT04D0301
Cytotoxicity against human 16HBE cells after 48 hrs by CCK-8 assay
Cytotoxicity against human 16HBE cells after 48 hrs by CCK-8 assay
[PMID: 31732254]
A-431 IC50
2.6 μM
Compound: Candesartan cilexetil
Inhibition of IDO in human A431 cells assessed as kynurenine production after 24 hrs
Inhibition of IDO in human A431 cells assessed as kynurenine production after 24 hrs
10.1039/C2MD00278G
A549 IC50
63.93 μM
Compound: 1; CDC, MT04D0301
Antiproliferative activity against human A549 cells measured after 48 hrs by CCK8 assay
Antiproliferative activity against human A549 cells measured after 48 hrs by CCK8 assay
[PMID: 31732254]
A549 IC50
65.92 μM
Compound: 1; CDC
Antiproliferative activity against human A549 cells incubated for 48 hrs by CCK-8 assay
Antiproliferative activity against human A549 cells incubated for 48 hrs by CCK-8 assay
[PMID: 33129593]
BEAS-2B IC50
79.76 μM
Compound: 1; CDC
Cytotoxicity against human BEAS-2B cells incubated for 48 hrs by CCK-8 assay
Cytotoxicity against human BEAS-2B cells incubated for 48 hrs by CCK-8 assay
[PMID: 33129593]
BEAS-2B IC50
89.94 μM
Compound: 1; CDC, MT04D0301
Cytotoxicity against human BEAS2B cells after 48 hrs by CCK-8 assay
Cytotoxicity against human BEAS2B cells after 48 hrs by CCK-8 assay
[PMID: 31732254]
EKVX IC50
> 100 μM
Compound: 1; CDC, MT04D0301
Antiproliferative activity against human EKVX cells measured after 48 hrs by CCK8 assay
Antiproliferative activity against human EKVX cells measured after 48 hrs by CCK8 assay
[PMID: 31732254]
HepG2 IC50
> 100 μM
Compound: 1; CDC, MT04D0301
Antiproliferative activity against human HepG2 cells measured after 48 hrs by CCK8 assay
Antiproliferative activity against human HepG2 cells measured after 48 hrs by CCK8 assay
[PMID: 31732254]
Huh-7 IC50
> 100 μM
Compound: 1; CDC, MT04D0301
Antiproliferative activity against human HuH7 cells measured after 48 hrs by CCK8 assay
Antiproliferative activity against human HuH7 cells measured after 48 hrs by CCK8 assay
[PMID: 31732254]
MCF7 IC50
> 100 μM
Compound: 1; CDC, MT04D0301
Antiproliferative activity against human MCF7 cells measured after 48 hrs by CCK8 assay
Antiproliferative activity against human MCF7 cells measured after 48 hrs by CCK8 assay
[PMID: 31732254]
MGC-803 IC50
57.14 μM
Compound: 1; CDC, MT04D0301
Antiproliferative activity against human MGC803 cells measured after 48 hrs by CCK8 assay
Antiproliferative activity against human MGC803 cells measured after 48 hrs by CCK8 assay
[PMID: 31732254]
MKN-45 IC50
68.87 μM
Compound: 1; CDC, MT04D0301
Antiproliferative activity against human MKN45 cells measured after 48 hrs by CCK8 assay
Antiproliferative activity against human MKN45 cells measured after 48 hrs by CCK8 assay
[PMID: 31732254]
NCI-H1299 IC50
45.02 μM
Compound: 1; CDC
Antiproliferative activity against human H1299 cells incubated for 48 hrs by CCK-8 assay
Antiproliferative activity against human H1299 cells incubated for 48 hrs by CCK-8 assay
[PMID: 33129593]
NCI-H1299 IC50
45.11 μM
Compound: 1; CDC, MT04D0301
Antiproliferative activity against human H1299 cells measured after 48 hrs by CCK8 assay
Antiproliferative activity against human H1299 cells measured after 48 hrs by CCK8 assay
[PMID: 31732254]
PLC IC50
60.21 μM
Compound: 1; CDC, MT04D0301
Antiproliferative activity against human PLC cells measured after 48 hrs by CCK8 assay
Antiproliferative activity against human PLC cells measured after 48 hrs by CCK8 assay
[PMID: 31732254]
T47D IC50
64.35 μM
Compound: 1; CDC, MT04D0301
Antiproliferative activity against human T47D cells measured after 48 hrs by CCK8 assay
Antiproliferative activity against human T47D cells measured after 48 hrs by CCK8 assay
[PMID: 31732254]
In Vitro

Candesartan Cilexetil (0.1-10 μM, 24 h) exhibits antiviral effects against ZIKV in HUVEC cells, HEK293T cells[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Viability Assay[1]

Cell Line: HUVEC cells, HEK293T cells
Concentration: 0.1 μM, 1 μM, 5 μM, 10 μM
Incubation Time: 24 h
Result: Showed a dose-dependent antiviral effect in ZIKV-infected HUVEC and HEK293T cells.
In Vivo

Candesartan Cilexetil (5 mg/kg, Oral gavage, once a day for 7 weeks) ameliorates myocardial remodeling and heart failure in Dahl salt-sensitive (DS) rats fed a high-salt diet[2].
Candesartan Cilexetil (1-10 mg/kg, Oral, once a day for 15 days) has an effect of skin wound healing in rats[3].
Candesartan Cilexetil (1-10 mg/kg, Administered through a stomach tube, once a day for 4-12 weeks) inhibits the increase in blood pressure in spontaneously hypertensive rats[5].
Candesartan Cilexetil (10 mg/kg, Oral, supplemented in drinking water, for 2-23 days) inhibits the synthesis of TGF-b1 and ameliorates the pulmonary fibrosis in bleomycin (HY-108345) induced pulmonary fibrosis model rats[6].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Dahl salt-sensitive hypertensive rats[2]
Dosage: 5 mg/kg
Administration: Oral gavage (p.o.)
Result: Increased body weight and decreased left ventricular end-diastolic diameter.
Decreased the level of iNOS mRNA and ADM mRNA in the left ventricle (LV).
Increased the eNOS protein mass in the LV and decreased the immunoreactive ADM contents of LV.
Enhanced immunoreactivity for eNOS.
Significantly decreased the degree of perivascular fibrosis.
Animal Model: Skin wound model rat [3]
Dosage: 1 mg/kg, 10 mg/kg
Administration: Oral
Result: Showed 100% re-epithelization of the wound at 1 mg/kg.
Significantly suppressed angiogenesis at 10 mg/kg.
Clinical Trial
Molecular Weight

610.66

Formula

C33H34N6O6

CAS No.
Appearance

Solid

Color

White to off-white

SMILES

O=C(C1=C2C(N=C(OCC)N2CC3=CC=C(C4=CC=CC=C4C5=NNN=N5)C=C3)=CC=C1)OC(OC(OC6CCCCC6)=O)C

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 2 years
-20°C 1 year
Solvent & Solubility
In Vitro: 

DMSO : ≥ 50 mg/mL (81.88 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent Mass 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
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

  • Protocol 1

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% Saline

    Solubility: ≥ 2.5 mg/mL (4.09 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

    Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
  • Protocol 2

    Add each solvent one by one:  10% DMSO    90% Corn Oil

    Solubility: ≥ 2.5 mg/mL (4.09 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

Purity & Documentation
References

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