Sertaconazole nitrate

SKU: orb1223465

Description

Sertaconazole nitrate is a topical broad-spectrum antifungal that is developed to provide an additional agent for the treatment of superficial cutaneous and mucosal infections.(In Vitro):Sertaconazole nitrate (0.03-40 μg/mL; 24 h) inhibits 150 strains of yeasts which includes six Candida species with arithmetic mean MIC of 0.77 μg/mL.Sertaconazole nitrate (1 μg/mL; 5, 10, 30, 60 min) activates p38 MAP kinase in a time-dependent manner.Sertaconazole nitrate (1, 2 μg/mL; 6, 8, or 24 h) increases a twofold release of PGE2 via COX-2 in keratinocytes, which is dependent on p38 activation.Sertaconazole nitrate (10, 20, 30, 40 μM; 24 h) induces strong mitotic arrest by depolymerizing interphase and spindle microtubules, thereby inducing chromosome aggregation defects and causing anti-proliferation effect.Sertaconazole nitrate (20, 40 μM; 24 h) induces apoptosis through p53 pathway in HeLa cells.Sertaconazole nitrate (20, 30 μM; 24, 48, and 72 h) inhibits the migration of HeLa cells in a concentration-dependent manner.Sertaconazole nitrate (15, 30 μM; 24 h) induces autophagy in A549, H460 cells.(In Vivo):Sertaconazole nitrate (1% (w/v); apply to the left ear, once) suppresses of TPA-induced ear edema CD-1 mice.

Key Properties

• CAS Number: 99592-39-9
• MW: 500.78
• Purity: >98% (HPLC)
• Formula: C₂₀H₁₅Cl₃N₂OS·HNO₃
• SMILES: O[N+]([O-])=O.ClC1=CC(Cl)=C(C=C1)C(CN1C=CN=C1)OCC1=CSC2=C1C=CC=C2Cl
• Target: Others
• Solubility: DMSO:100 mg/mL (199.68 mM); Ethanol:<1 mg/mL (<1 mM); Water:<1 mg/mL (<1 mM)

Bioactivity

• In Vivo:
  Sertaconazole nitrate (1% (w/v); apply to the left ear, once) suppresses of TPA-induced ear edema CD-1 mice. Animal model: CD-1 mice (TPA-induced ear edema model). Dosage: 1% (w/v). Administration: Apply to the left ear, once. Result: Exhibited a significant reduction of inflammation in mice by mediating PGE2 release.
• In Vitro:
  Sertaconazole nitrate (0.03-40 μg/mL; 24 h) inhibits 150 strains of yeasts which includes six Candida species with arithmetic mean MIC of 0.77 μg/mL. Sertaconazole nitrate (1 μg/mL; 5, 10, 30, 60 min) activates p38 MAP kinase in a time-dependent manner. Sertaconazole nitrate (1, 2 μg/mL; 6, 8, or 24 h) increases a twofold release of PGE2 via COX-2 in keratinocytes, which is dependent on p38 activation. Sertaconazole nitrate (10, 20, 30, 40 μM; 24 h) induces strong mitotic arrest by depolymerizing interphase and spindle microtubules, thereby inducing chromosome aggregation defects and causing anti-proliferation effect. Sertaconazole nitrate (20, 40 μM; 24 h) induces apoptosis through p53 pathway in HeLa cells. Sertaconazole nitrate (20, 30 μM; 24, 48, and 72 h) inhibits the migration of HeLa cells in a concentration-dependent manner. Sertaconazole nitrate (15, 30 μM; 24 h) induces autophagy in A549, H460 cells. Cell Viability Assay Cell line: C. albicans, C. guilliermondii, C. krusei, C. parapsilosi, C. tropicalis, C. glabrata Concentration: 0.03-40 μg/mL Incubation time: 24 h. Result: Againsted 150 strains of yeasts (six Candida species) which included C. albicans, C. guilliermondii, C. krusei, C. parapsilosi, C. tropicalis, C. glabrata species with arithmetic mean MIC values of 1.02, 0.51, 0.38, 0.31, 1.67 and 0.78 μg/mL, respectively. Western blot analysis. Cell line: HaCaT cells. Concentration: 1 μg/mL. Incubation time: 5, 10, 30, 60 min. Result: Showed activity of activating p38 MAP kinase and Hsp27 in a time-dependent manner. Western blot analysis. Cell line: HaCaT cells. Concentration: 1, 2 μg/mL. Incubation time: 6 or 8 h. Result: Induced 50% expression of COX-2 and resulted in a twofold increased in PGE2 release. Western blot analysis. Cell line: siRNA-transfected HaCaT cells (without p38 MAP kinase expression). Concentration: 1 μg/mL. Incubation time: 24 h. Result: Mediated induction of PGE2 was dependent on p38 activation. Cell Proliferation Assay Cell line: HeLa, HEK-293, MCF-7, A549 cells. Concentration: 0-100 μM. Incubation time: 24 h. Result: Showed antiproliferation activity with IC50s of 38, 45.1, 41.5, and 40.8 μM for HeLa, HEK-293, A549, and MCF-7 cells, respectively.

Storage & Handling

• Storage: Storage temperature: -20°C. Stability: ≥ 2 years
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

FI-7045

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