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Sertaconazole nitrate Fungal inhibitor

Sertaconazole nitrate (FI-7045,FI7056) is a topical broad-spectrum antifungal that is developed to provide an additional agent for the treatment of superficial cutaneous and mucosal infections.

Sertaconazole nitrate Fungal inhibitor Chemical Structure

Chemical Structure

Molecular Weight: 500.78

Purity & Quality Control

Batch: S316101 DMSO]100 mg/mL]false]Water]Insoluble]false]Ethanol]Insoluble]false Purity: 99.75%
99.75

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Mechanism of Action

In vitro
In vitro

Sertaconazole nitrate reduces the release of cytokines from activated lymphocytes and mitigated inflammation in animal models of irritant contact dermatitis and neurogenic inflammation in a dose-dependent fashion. This compound is found to inhibit the proliferation of stimulated human lymphocytes with IC50 of 4 μg/mL. [1] It inhibits ergosterol synthesis by blockade of the P450-dependent enzyme pathway that catalyzes the methylation of lanosterol to ergosterol, thus inhibits fungal cell growth. This chemical binds directly to nonsterol lipids in the membrane, which interferes with the regulation of the permeability of fungal cell membranes, thus induces fungal cell death. [2] This compound (< 100 μg/mL) activates p38 MAP kinase and Hsp27 in keratinocytes. It induces (< 2 μg/mL) COX-2 protein expression and PGE2 production in keratinocytes, which dependent on p38 activation. PGE2 is involved in this compound (1 μg/mL)-mediated suppression of cytokine production in keratinocytes and PBMCs. [3]

In Vivo
In vivo

The mean ear weight of Tetradecanoyl phorbol acetate (TPA)-challenged murine treated with sertaconazole nitrate (1%) is 7.23 mg compared with 14.7 mg for controls, indicating a statistically significant reduction in irritant dermatitis. This compound elicits a significant reduction in Resiniferatoxin-induced ear edema when compared with controls in CD-1 mice. Topical treatment with this chemical significantly inhibits contact hypersensitivity and decreases the content of the pro-inflammatory cytokines TNFα, IL-2, and IFNγ in oxazolone exposed murine skin. [1] Clinical trials with this compound cream 2% show efficacy in the treatment of superficial cutaneous fungal infections. [2] It reduces inflammation via inducing PGE2 production and the COX-2 inhibitor blocks it from exerting its anti-inflammatory effects in a mouse model of TPA-induced ear edema. [3] The dermal administration of this chemical to rats, in which edema is induced by application of croton oil in the external ear, induced a 39.8% reduction of edema. [4]
NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT00856596 Unknown status
Tinea Pedis|Athlete''s Foot|Foot Fungus|Ringworm
Jamaica Hospital Medical Center|Johnson & Johnson
 March 2009 Phase 3

References
  • https://pubmed.ncbi.nlm.nih.gov/16868738/
  • https://pubmed.ncbi.nlm.nih.gov/16822638/
  • https://pubmed.ncbi.nlm.nih.gov/17637821/
  • https://pubmed.ncbi.nlm.nih.gov/8803954/

Chemical Information

Molecular Weight 500.78 Formula

C20H15Cl3N2OS.HNO3

 
CAS No. 99592-39-9 SDF Download SDF
Synonyms FI-7045,FI7056
Smiles C1=CC2=C(C(=C1)Cl)SC=C2COC(CN3C=CN=C3)C4=C(C=C(C=C4)Cl)Cl.[N+](=O)(O)[O-]

Storage and Stability

Storage (From the date of receipt)

In vitro
Batch:

DMSO : 100 mg/mL ( (199.68 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Water : Insoluble

Ethanol : Insoluble


Molecular Weight Calculator

In vivo
Batch:

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In vivo Formulation Calculator

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In vivo Formulation Calculator (Clear solution)

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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid 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 master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
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Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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