Naftifine hydrochloride

SKU: orb1308252

Description

Naftifine hydrochloride is a synthetic allylamine antifungal agent that acts by inhibiting squalene epoxidase, disrupting ergosterol biosynthesis and leading to squalene accumulation in fungal cells. It is used in research for studying antifungal mechanisms and has demonstrated efficacy in both in vitro assays and in vivo models of dermatophyte and yeast infections.

Research Area

Infectious Disease & Virology, Pharmacology & Drug Discovery, Stem Cell & Developmental Biology

Key Properties

• CAS Number: 65473-14-5
• MW: 323.86
• Purity: 99.84% (May vary between batches)
• Formula: C₂₁H₂₂ClN
• SMILES: Cl.CN(C\C=C\c1ccccc1)Cc1cccc2ccccc12
• Target: Hedgehog/Smoothened,Antibiotic,Antifungal
• Solubility: DMSO:100 mg/mL (308.78 mM);10% DMSO+40% PEG300+5% Tween 80+45% Saline:4 mg/mL (12.35 mM);H2O:2.5 mg/mL (7.72 mM);Ethanol:8 mg/mL (24.7 mM)

Bioactivity

• In Vivo:
  Naftifine HCl 2% cream results in clinical cure rate and clinical success rate of 33% and 84% after treatment for 4 weeks, and week 2 efficacy response rates in Naftifine HCl 2% subjects are all lower than at week 4 but are significantly higher than week 2 vehicle-treated counterparts. Naftifine causes interruption of fungal ergosterol synthesis and accumulation of squalene in fungal organisms. Naftifine also has demonstrated anti-inflammatory properties such as a reduction in superoxide production and a reduction in polymorphonuclear leukocyte chemotaxis/endothelial adhesion. Naftifine has shown good efficacy and safety for a variety of conditions and is a useful treatment that provides both antifungal action and relief of inflammatory signs and symptoms. Few adverse events have been noted with naftifine use, the most frequent being mild and transient burning, stinging, or itching in the application area.
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• In Vitro:
  Naftifine demonstrates a broad in vitro activity spectrum against dermatophytes (38 strains; MIC 0.1 to 0.2 mg/mL), aspergilli (6 strains; MIC 0.8 to 12.5 mg/mL), Sporothrix schenckii (2 strains; MIC 0.8 and 1.5 mg/mL), and Candida yeasts (77 strains; MIC 1.5 to >100 mg/mL). For C. albicans Δ63, the MIC is 100 mg/L in Sabouraud medium (initial pH 6.5). At 50 mg/L, naftifine inhibits sterol biosynthesis by over 99% in both whole cells and cell extracts of C. albicans. Its primary mode of action is blocking fungal squalene epoxidation.
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Storage & Handling

• Storage: -20°C
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

corporis, cruris, dermatophytes, Antibiotic, Exoderil, Fungal, Inhibitor, Hedgehog, Naftifine, Naftifine HCl, Naftifine Hydrochloride, Naftifine hydrochloride, Naftifungin, Naftin, inhibit, pedis, tinea, Smoothened

Compound Identifiers

PubChem CID

5281098