Home Microbiology Fungal inhibitor Sertaconazole nitrate

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Sertaconazole nitrate Fungal inhibitor

Cat.No.S3161

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

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Quality Control

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

Solubility

In vitro
Batch:

DMSO : 100 mg/mL (199.68 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Water : Insoluble

Ethanol : Insoluble

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Chemical Information, Storage & Stability

Molecular Weight 500.78 Formula

C20H15Cl3N2OS.HNO3

 
 Storage (From the date of receipt)
CAS No. 99592-39-9 Download SDF Storage of Stock Solutions

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-]

Mechanism of Action

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. 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. 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.

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. Clinical trials with this compound cream 2% show efficacy in the treatment of superficial cutaneous fungal infections. 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. 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.

References
  • [4] https://pubmed.ncbi.nlm.nih.gov/8803954/

Clinical Trial Information

(data from https://clinicaltrials.gov, updated on 2024-05-22)

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

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