Cat. No.: HY-B0736

Sertaconazole

(Synonyms: FI7056 free base)

2 Cited Publications

Customer Review

Based on 2 publication(s) in Google Scholar

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

For research use only. We do not sell to patients.

Purity: 99.42%
CAS No.: 99592-32-2
Formula: C₂₀H₁₅Cl₃N₂OS
Molecular Weight:437.77

Storage:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month

Sertaconazole Chemical Structure

CAS No.: 99592-32-2

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Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biological Activity
- Description
- In Vitro
- In Vivo
- Clinical Trial
Chemical Information
Publications (2)
Solvent & Solubility
- In Vitro
- In Vivo
Purity & Documentation
References
Help & FAQs
Bioz

Biological Activity

Description

All p38 MAPK Isoforms :

In Vitro

Sertaconazole (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 (1 µg/mL; 5, 10, 30, 60 min) activates p38 MAP kinase in a time-dependent manner^[2].
Sertaconazole (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].
Cetaconazole (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 (20, 40 µM; 24 h) induces apoptosis through p53 pathway in HeLa cells^[3].
Sertaconazole (20, 30 µM; 24, 48, and 72 h) inhibits the migration of HeLa cells in a concentration-dependent manner^[3].
Sertaconazole (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/m
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 (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.

Clinical Trial

NCT Number	Sponsor	Condition	Start Date	Phase A549
NCT01329991	Plexxikon\|		2011-05	PHASE1

Chemical Information

CAS No. 99592-32-2
Appearance Solid
Molecular Weight 437.77
Formula C₂₀H₁₅Cl₃N₂OS
Color White to off-white
SMILES

ClC1=CC=C(C(OCC2=CSC3=C(Cl)C=CC=C32)CN4C=CN=C4)C(Cl)=C1
Synonyms

FI7056 free base
Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

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

Solvent & Solubility

In Vitro:

DMSO : 25 mg/mL (57.11 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

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

2.2843 mL

11.4215 mL

22.8430 mL

5 mM

0.4569 mL

2.2843 mL

4.5686 mL

10 mM

0.2284 mL

1.1422 mL

2.2843 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. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Molarity Calculator

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

Mass Mass

Concentration Concentration

Volume Volume

Molecular Weight Molecular Weight

Dilution Calculator

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

Concentration _(start) Concentration _(start)

Volume _(start) Volume _(start)

Concentration _(final) Concentration _(final)

Volume _(final) Volume _(final)

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 (5.71 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 (5.71 mM); Suspended solution; Need ultrasonic

This protocol yields a suspended solution of 2.5 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.

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 (5.71 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

Purity & Documentation

Select Batch:

Purity: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (290 KB)
SDS (394 KB)
- English - EN (394 KB)
- Français - FR (394 KB)
- Deutsch - DE (394 KB)
- Norwegian - NO (394 KB)
- Español - ES (394 KB)
- Swedish - SV (394 KB)
- Italian - IT (394 KB)
- Portuguese - PT (394 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)

References

[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

Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	2.2843 mL	11.4215 mL	22.8430 mL	57.1076 mL
	5 mM	0.4569 mL	2.2843 mL	4.5686 mL	11.4215 mL
	10 mM	0.2284 mL	1.1422 mL	2.2843 mL	5.7108 mL
	15 mM	0.1523 mL	0.7614 mL	1.5229 mL	3.8072 mL
	20 mM	0.1142 mL	0.5711 mL	1.1422 mL	2.8554 mL
	25 mM	0.0914 mL	0.4569 mL	0.9137 mL	2.2843 mL
	30 mM	0.0761 mL	0.3807 mL	0.7614 mL	1.9036 mL
	40 mM	0.0571 mL	0.2855 mL	0.5711 mL	1.4277 mL
	50 mM	0.0457 mL	0.2284 mL	0.4569 mL	1.1422 mL

Sertaconazole

2 Cited Publications

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Sertaconazole

Anti-Infection Compound Library

Apoptosis Compound Library

Cell Cycle/DNA Damage Compound Library

Immunology/Inflammation Compound Library

MAPK Compound Library

FDA-Approved Drug Library

Anti-Cancer Compound Library

Autophagy Compound Library

Anti-Aging Compound Library

Drug Repurposing Compound Library

Oxygen Sensing Compound Library

Antifungal Compound Library

NMPA-Approved Drug Library

Pyroptosis Compound Library

Cytoskeleton Compound Library

FDA Approved & Pharmacopeial Drug Library

Anti-Lung Cancer Compound Library

Anti-Cancer Metabolism Compound Library

Neurodegenerative Disease-related Compound Library

Angiogenesis-Related Compound Library

Protein-protein Interaction Inhibitor Library

FDA-Approved Anticancer Drug Library

Human Metabolite Library

Osteogenesis Compound Library

Heterocyclic Compound Library

Pain-Related Compound Library

Off-patent Drug Library

Cell Death Library

Multi-Target Compound Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Drug Repurposing Compound Library Plus

FDA-Approved Drug Library Plus

FDA-Approved Drug Library Mini

Bioactive Compound Library

Protein Kinase Compound Library

Non-Alcoholic Fatty Liver Disease (NAFLD) Compound Library

Cell Proliferation Compound Library

High-Throughput Bioactive Compound Library

Mass Spectrometry Human Metabolite Library

High-Efficiency Gene Editing Compound Library

Lactylation Compound Library

Publications Citing Use of MedChemExpress (MCE) Sertaconazole

All p38 MAPK Isoforms

Biological Activity

Chemical Information

Publications (2)

Solvent & Solubility

Purity & Documentation

References

Help & FAQs

Complete Stock Solution Preparation Table

Sertaconazole Related Classifications

Cat. No.: HY-B0736