Art. -Nr.: HY-B0736A

Sertaconazole nitrate

(Synonyms: FI7056)

2 Cited Publications

Kundenbewertung

Based on 2 publication(s) in Google Scholar

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.

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Reinheit: 99.19%
CAS. Nr.: 99592-39-9
Formel: C₂₀H₁₆Cl₃N₃O₄S
Molecular Weight:500.78

Speicherung:

4°C, sealed storage, away from moisture

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

Sertaconazole nitrate Chemical Structure

CAS. Nr.: 99592-39-9

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Biologische Aktivität
- Beschreibung
- In Vitro
- In Vivo
Chemical Information
Publications (2)
Lösungsmittel & Löslichkeit
- In Vitro
- In Vivo
Reinheit & Dokumentation
Verweise
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

Alle p38 MAPK Isoform-spezifische Produkte anzeigen :

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.

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.

Chemical Information

CAS. Nr. 99592-39-9
Appearance Solid
Molecular Weight 500.78
Formel C₂₀H₁₆Cl₃N₃O₄S
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
Synonyms

FI7056
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)

Publications (2)

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Journal Impact Factor

J Exp Clin Cancer Res

Sertaconazole-repurposed nanoplatform enhances lung cancer therapy via CD44-targeted drug delivery. [Abstract]

2023 Jul 29;42(1):188. PMID: 37507782
MedComm (2020)

Sertaconazole provokes proapoptotic autophagy via stabilizing TRADD in nonsmall cell lung cancer cells. [Abstract]

2021 Dec 16;2(4):821-837. PMID: 34977879

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.

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

1.9969 mL

9.9844 mL

19.9688 mL

5 mM

0.3994 mL

1.9969 mL

3.9938 mL

10 mM

0.1997 mL

0.9984 mL

1.9969 mL

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.

Molaritätsrechner

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

In Vivo:

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

Stock Solution Working Solution

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.

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.

Protocol 3

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

Solubility: ≥ 2.5 mg/mL (4.99 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.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
Saline +

The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Working solution concentration: 0.22 mg/mL

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (290 KB)
SDS (419 KB)
- English - EN (419 KB)
- Français - FR (419 KB)
- Deutsch - DE (419 KB)
- Norwegian - NO (419 KB)
- Español - ES (419 KB)
- Swedish - SV (419 KB)
- Italian - IT (419 KB)
- Korean - KR (419 KB)
- Portuguese - PT (419 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

Verweise

[1]. Carrillo-Muñoz AJ, et al. In-vitro antifungal activity of sertaconazole, econazole, and bifonazole against Candida spp. J Antimicrob Chemother. 1995 Oct;36(4):713-6. [Content Brief]

[2]. Sur R, et al. Anti-inflammatory activity of sertaconazole nitrate is mediated via activation of a p38-COX-2-PGE2 pathway. J Invest Dermatol. 2008 Feb;128(2):336-44. [Content Brief]

[3]. Sebastian J, et al. Sertaconazole induced toxicity in HeLa cells through mitotic arrest and inhibition of microtubule assembly. Naunyn Schmiedebergs Arch Pharmacol. 2021 Jun;394(6):1231-1249. [Content Brief]

[4]. Zhang W, et al. Sertaconazole provokes proapoptotic autophagy via stabilizing TRADD in nonsmall cell lung cancer cells. MedComm (2020). 2021 Dec 16;2(4):821-837. [Content Brief]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	1.9969 mL	9.9844 mL	19.9688 mL	49.9221 mL
	5 mM	0.3994 mL	1.9969 mL	3.9938 mL	9.9844 mL
	10 mM	0.1997 mL	0.9984 mL	1.9969 mL	4.9922 mL
	15 mM	0.1331 mL	0.6656 mL	1.3313 mL	3.3281 mL
	20 mM	0.0998 mL	0.4992 mL	0.9984 mL	2.4961 mL
	25 mM	0.0799 mL	0.3994 mL	0.7988 mL	1.9969 mL
	30 mM	0.0666 mL	0.3328 mL	0.6656 mL	1.6641 mL
	40 mM	0.0499 mL	0.2496 mL	0.4992 mL	1.2481 mL
	50 mM	0.0399 mL	0.1997 mL	0.3994 mL	0.9984 mL
	60 mM	0.0333 mL	0.1664 mL	0.3328 mL	0.8320 mL
	80 mM	0.0250 mL	0.1248 mL	0.2496 mL	0.6240 mL
	100 mM	0.0200 mL	0.0998 mL	0.1997 mL	0.4992 mL

Sertaconazole nitrate

2 Cited Publications

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Sertaconazole nitrate

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Publications Citing Use of MedChemExpress (MCE) Sertaconazole nitrate

Alle p38 MAPK Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Publications (2)

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

Sertaconazole nitrate Related Classifications

HY-B0736A Related Classifications