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Sertaconazole nitrate

Catalog No. T6665   CAS 99592-39-9
Synonyms: FI-7045, Ginedermofix, FI7056, Ertaczo

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

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Sertaconazole nitrate Chemical Structure
Sertaconazole nitrate, CAS 99592-39-9
Pack Size Availability Price/USD Quantity
10 mg In stock $ 38.00
25 mg In stock $ 48.00
50 mg In stock $ 66.00
100 mg In stock $ 98.00
200 mg In stock $ 189.00
1 mL * 10 mM (in DMSO) In stock $ 39.00
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Purity: 98.66%
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Biological Description
Chemical Properties
Storage & Solubility Information
Description Sertaconazole nitrate (FI-7045), a topical broad-spectrum antifungal, is developed to supply an additional agent for the treatment of superficial cutaneous and mucosal infections.
Targets&IC50 Proliferation (human lymphocytes):4 μg/mL
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. Sertaconazole nitrate is found to inhibit the proliferation of stimulated human lymphocytes with IC50 of 4 μg/mL. [1] Sertaconazole nitrate inhibits ergosterol synthesis by blockade of the P450-dependent enzyme pathway that catalyzes the methylation of lanosterol to ergosterol, thus inhibits fungal cell growth. Sertaconazole nitrate 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] Sertaconazole nitrate (< 100 μg/mL) activates p38 MAP kinase and Hsp27 in keratinocytes. Sertaconazole induces (< 2 μg/mL) COX-2 protein expression and PGE2 production in keratinocytes, which dependent on p38 activation. PGE2 is involved in sertaconazole (1 μg/mL)-mediated suppression of cytokine production in keratinocytes and PBMCs. [3]
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. Sertaconazole nitrate 1% elicits a significant reduction in Resiniferatoxin-induced ear edema when compared with controls in CD-1 mice. Topical treatment with sertaconazole nitrate 1% 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 sertaconazole nitrate cream 2% show efficacy in the treatment of superficial cutaneous fungal infections. [2] Sertaconazole reduces inflammation via inducing PGE2 production and the COX-2 inhibitor blocks sertaconazole from exerting its anti-inflammatory effects in a mouse model of TPA-induced ear edema. [3] The dermal administration of sertaconazole nitrate (2%) to rats, in which edema is induced by application of croton oil in the external ear, induced a 39.8% reduction of edema. [4]
Synonyms FI-7045, Ginedermofix, FI7056, Ertaczo
Molecular Weight 500.78
Formula C20H15Cl3N2OS·HNO3
CAS No. 99592-39-9

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 93 mg/mL (185.7 mM)

H2O: < 1 mg/mL (insoluble or slightly soluble)

Ethanol: < 1 mg/mL (insoluble or slightly soluble)

TargetMolReferences and Literature

1. Liebel F, et al. Arch Dermatol Res, 2006, 298(4), 191-199. 2. Pfaller MA, et al. Diagn Microbiol Infect Dis, 2006, 56(2), 147-152. 3. Sur R, et al. J Invest Dermatol, 2008, 128(2), 336-344. 4. Agut J, et al. Methods Find Exp Clin Pharmacol, 1996, 18(4), 233-234.

Related compound libraries

This product is contained In the following compound libraries:
Drug Repurposing Compound Library Anti-Fungal Compound Library Approved Drug Library Bioactive Compound Library NO PAINS Compound Library Clinical Compound Library Anti-Infection Compound Library Antibiotics Library Antidepressant Compound Library FDA-Approved & Pharmacopeia Drug Library

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Keywords

Sertaconazole nitrate 99592-39-9 Microbiology/Virology Antifungal Antibiotic COX-2 FI-7056 Inhibitor inhibit MCF-7 HaCaT Candida HeLa FI-7045 Ginedermofix FI7056 Ertaczo p38 MAPK A549 PGE2 Sertaconazole HEK-293 Apoptosis FI 7045 FI 7056 Fungal Microtubule/Tubulin FI7045 Sertaconazole Nitrate Autophagy inhibitor

 

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