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> Sertaconazole (nitrate) [99592-39-9]

Sertaconazole (nitrate) [99592-39-9]

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Katalog-Nummer HY-B0736A-1mL

Size : 10mM/1mL

Marke : MedChemExpress


Beschreibung

Sertaconazole nitrate (FI7056) is a broad-spectrum topical antifungal agent, exhibits anti-inflammatory activity via activation of a p38-COX-2-PGE2 pathway. Sertaconazole nitrate is also a microtubule inhibitor, shows antiproliferative effect, induces apoptosis and autophagy, and can also inhibit the migration of cells[1][2][3][4].

In Vitro

Sertaconazole nitrate (0.03-40 μg/mL; 24 h) inhibits 150 strains of yeasts which includes six Candida species with arithmetic mean MIC of 0.77 μg/mL[1].
Sertaconazole nitrate (1 μg/mL; 5, 10, 30, 60 min) activates p38 MAP kinase in a time-dependent manner[2].
Sertaconazole nitrate (1, 2 μg/mL; 6, 8, or 24 h) increases a twofold release of PGE2 via COX-2 in keratinocytes, which is dependent on p38 activation[2].
Sertaconazole nitrate (10, 20, 30, 40 μM; 24 h) induces strong mitotic arrest by depolymerizing interphase and spindle microtubules, thereby inducing chromosome aggregation defects and causing anti-proliferation effect[3].
Sertaconazole nitrate (20, 40 μM; 24 h) induces apoptosis through p53 pathway in HeLa cells[3].
Sertaconazole nitrate (20, 30 μM; 24, 48, and 72 h) inhibits the migration of HeLa cells in a concentration-dependent manner[3].
Sertaconazole nitrate (15, 30 μM; 24 h) induces autophagy in A549, H460 cells[4].

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

Sertaconazole nitrate Related Antibodies

Cell Viability Assay[1]

Cell Line: C. albicans, C. guilliermondii, C. krusei, C. parapsilosi, C. tropicalis, C. glabrata
Concentration: 0.03-40 µg/mL
Incubation Time: 24 h
Result: Againsted 150 strains of yeasts (six Candida species) which included C. albicans, C. guilliermondii, C. krusei, C. parapsilosi, C. tropicalis, C. glabrata species with arithmetic mean MIC values of 1.02, 0.51, 0.38, 0.31, 1.67 and 0.78 µg/mL, respectively.

Western Blot Analysis[2]

Cell Line: HaCaT cells
Concentration: 1 µg/mL
Incubation Time: 5, 10, 30, 60 min
Result: Showed activity of activating p38 MAP kinase and Hsp27 in a time-dependent manner.

Western Blot Analysis[2]

Cell Line: HaCaT cells
Concentration: 1, 2 µg/mL
Incubation Time: 6 or 8 h
Result: Induced 50% expression of COX-2 and resulted in a twofold increased in PGE2 release.

Western Blot Analysis[2]

Cell Line: siRNA-transfected HaCaT cells (without p38 MAP kinase expression)
Concentration: 1 µg/mL
Incubation Time: 24 h
Result: Mediated induction of PGE2 was dependent on p38 activation.

Cell Proliferation Assay[3]

Cell Line: HeLa, HEK-293, MCF-7, A549 cells
Concentration: 0-100 µM
Incubation Time: 24 h
Result: Showed antiproliferation activity with IC50s of 38, 45.1, 41.5, and 40.8 μM for HeLa, HEK-293, A549, and MCF-7 cells, respectively.
Exhibited mitotic block activity and induced cell death at concentration above 30 μM, but no significant increased in the number of mitotic cells.
Depolymerized interphase and spindle microtubules inducing defect in chromosomal congression.

Apoptosis Analysis[3]

Cell Line: HeLa cells
Concentration: 10, 20, 40 µM
Incubation Time: 24 h
Result: Induced approximately 5%, 10%, and 21% cells apoptotic at concentrations of 10, 20 and 40 μM, respectively.

Western Blot Analysis[3]

Cell Line: A549 cells
Concentration: 20, 40 µM
Incubation Time: 24 h
Result: Induced apoptosis through p53 pathway that the expression of p53 from 30% to 50% and 95% and p21 from 11 to 39% and 40% respectively.
Resulted in Noxa and Puma, two direct transcriptional targets of p53 to be overexpressed.

Cell Migration Assay [3]

Cell Line: HeLa cells
Concentration: 20, 30 µM
Incubation Time: 24, 48, and 72 h
Result: Inhibited the migration of HeLa cells at concentrations lesser than its IC50, which in a concentration-dependent manner.

Cell Autophagy Assay[4]

Cell Line: A549, H460 cells
Concentration: 15, 30 µM
Incubation Time: 24 h
Result: Increased endogenous LC3 puncta and LC3 intensity, which indicated induction of autophagy in A549 and H460 cells.
In Vivo

Sertaconazole nitrate (1% (w/v); apply to the left ear, once) suppresses of TPA-induced ear edema CD-1 mice[2].

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

Animal Model: CD-1 mice (TPA-induced ear edema model)[2].
Dosage: 1% (w/v)
Administration: Apply to the left ear, once.
Result: Exhibited a significant reduction of inflammation in mice by mediating PGE2 release.
Klinische Studie
Molekulargewicht

500.78

Formel

C20H16Cl3N3O4S
CAS. Nr.
Appearance

Solid

Color

White to off-white

SMILES

ClC1=CC=C(C(OCC2=CSC3=C(Cl)C=CC=C32)CN4C=CN=C4)C(Cl)=C1.O[N+]([O-])=O
Versand

Room temperature in continental US; may vary elsewhere.
Speicherung

4°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

Lösungsmittel & Löslichkeit
In Vitro: 

DMSO : ≥ 100 mg/mL (199.69 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 1.9969 mL 9.9844 mL 19.9688 mL
5 mM 0.3994 mL 1.9969 mL 3.9938 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, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

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 (4.99 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% (20% SBE-β-CD in Saline)

    Solubility: ≥ 2.5 mg/mL (4.99 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 900 μL 20% SBE-β-CD in Saline, and mix evenly.

    Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
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