Molecular Formula | C20H15Cl3N2OS.HNO3 |
Molar Mass | 500.78 |
Melting Point | 158-160° |
Solubility | DMSO: soluble20mg/mL, clear |
Appearance | powder |
Color | white to beige |
pKa | pKb: 7.26(at 25℃) |
Storage Condition | -20°C |
In vitro study | Sertaconazole nitrate can reduce the release of cytokines in activated lymphocytes and reduce the inflammatory response in animal models of irritant contact dermatitis and neurogenic inflammation, and this effect has a dose-dependent nature. Sertaconazole nitrate was shown to inhibit the proliferation of stimulated human lymphocytes with an IC50 of 4 μg/mL . P450 dependent enzyme activity pathway can methylate lanosterol to form ergosterol ,Sertaconazole nitrate inhibits the synthesis of ergosterol by blocking this pathway to inhibit the growth of fungal cells. Sertaconazole nitrate can directly bind to non-Sterol lipids on the cell membrane to interfere with the regulation of fungal cell membrane permeability and induce fungal death. Sertaconazole nitrate (< 100 μg/mL) can activate p38 protein kinase and Hsp27 in keratinocytes. Sertaconazole (< 2 μg/mL) induces COX-2 protein expression and PGE2 production in keratinocytes, a process dependent on p38 activation. Involvement of PGE2 in sertaconazole (1 μg/mL)-mediated inhibition of cytokine production in keratinocytes and peripheral monocytes |
In vivo study | The average ear weight of Sertaconazole nitrogen (1%)-treated mice after Tetradecanoyl phorbol acetate (TPA) stimulation was 7.23 mg, compared with 14.7 mg in the control group, indicating a significant reduction in the symptoms of irritant dermatitis. In CD-1 mice, 1% Sertaconazole nitrogen significantly reduced the symptoms of ear edema induced by Resiniferatoxin compared with the control group. 1% Sertaconazole nitrate topical treatment significantly inhibited contact allergic reactions and reduced the content of pro-inflammatory cytokines TNFα, IL-2 and IFNγ in the skin of mice exposed to oxazolone. Clinical trials have shown that 2% Sertaconazole nitrate cream can treat superficial skin fungal infections. In TPA-induced mouse ear edema model, Sertaconazole exerts anti-inflammatory effects by inducing PGE2 production and COX-2 inhibitor to relieve inflammatory symptoms. In a croton oil-induced rat model of external ear edema, cutaneous administration of Sertaconazole nitrate (2%) resulted in a 39.8% reduction in edema |
WGK Germany | 3 |