| Size | Price | Stock | Qty |
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| 50mg |
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| 100mg |
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| 250mg |
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| 500mg |
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| 1g |
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| Other Sizes |
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Purity: ≥98%
Sertaconazole nitrate (Ertaczo, Dermofix, Konzert, and Zalain) is a topical broad-spectrum antifungal medication of the imidazole class. It is available as a cream to treat skin infections such as athlete's foot. Sertaconazole was developed to provide an additional agent for the treatment of superficial cutaneous and mucosal infections. Sertaconazole nitrate may also inhibit endogenous respiration, interact with membrane phospholipids, inhibit the transformation of yeasts to mycelial forms, inhibit purine uptake, and impair triglyceride and/or phospholipid biosynthesis.
| ln Vitro |
Sertaconazole nitrate (0.03-40 µg/mL; 24 hours) inhibits 150 yeast strains, with an arithmetic mean MIC of 0.77 µg/mL, including six species of Candida [1]. Sertaconazole nitrate (1 µg/mL; 5, 10, 30, 60 minutes) has a time-dependent effect on p38 MAP kinase activation [2]. Dependent on p38 activation, sertaconazole nitrate (1, 2 µg/mL; 6, 8, or 24 hours) doubles PGE2 release via COX-2 in keratinocytes [2]. By depolymerizing interphase and spindle microtubules, sertaconazole nitrate (10, 20, 30, 40 µM; 24 h) promotes a significant mitotic arrest, resulting in chromosomal aggregation abnormalities and anti-proliferative effects [3]. Using the p53 pathway, sertaconazole nitrate (20, 40 µM; 24 hours) causes apoptosis in HeLa cells [3]. HeLa cell migration is inhibited by sertaconazole nitrate (20, 30 µM; 24, 48, and 72 hours) in a concentration-dependent manner [3]. In A549 and H460 cells, sertaconazole nitrate (15, 30 µM; 24 hours) can cause autophagy [4].
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| ln Vivo |
In CD-1 mice, tetraconazole nitrate (1% (w/v); administered once to the left ear) can prevent ear edema caused by TPA [2].
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| Cell Assay |
Cell Viability Assay[1]
Cell Types: Candida albicans, Candida quillimoniensis, Candida krusei, Candida parapsilosis, Candida tropicalis, Candida glabrata Tested Concentrations: 0.03-40 µg/mL Incubation Duration: 24 hrs (hours) Experimental Results: Against 150 strains of yeast (six species of Candida), including Candida albicans, Candida quillimoniensis, Candida krusei, Candida parapsilosis, Candida tropicalis, and Candida glabrata, the arithmetic mean MIC value is 1.02 , 0.51, 0.38, 0.31, 1.67 and 0.78 are micrograms/ml respectively. Western Blot Analysis[2] Cell Types: HaCaT cells Tested Concentrations: 1 µg/mL Incubation Duration: 5, 10, 30, 60 minutes Experimental Results: demonstrated activity to activate p38 MAP kinase and Hsp27 in a time-dependent manner. Western Blot Analysis[2] Cell Types: HaCaT cells Tested Concentrations: 1, 2 µg/mL Incubation Duration: 6 or 8 hrs (hours) Experimental Results: Induced COX-2 expression by 50%, resulting in a twofold increase in PGE2 release. Western Blot Analysis[2] Cell Types: siRNA-transfected HaCaT cells (no p38 MAP kinase expressio |
| Animal Protocol |
Animal/Disease Models: CD-1 mice (TPA-induced ear edema model) [2].
Doses: 1% (w/v) Route of Administration: Apply to left ear once. Experimental Results: Dramatically diminished inflammation in mice by mediating PGE2 release. |
| References |
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| Additional Infomation |
Sertaconazole Nitrate is the nitrate salt form of sertaconazole, a synthetic imidazole derivative with antifungal property. Sertaconazole nitrate inhibits fungal cytochrome P-450 sterol C-14 alpha-demethylation, resulting in the accumulation of fungal 14 alpha-methyl sterols and the inhibition of ergosterol synthesis, an essential component of the cell membrane of fungi. This leads to a disruption of cell membrane permeability and leakage of adenine triphosphate (ATP) and other constituents from fugal cells.
See also: Sertaconazole (has active moiety). |
| Molecular Formula |
C20H16CL3N3O4S
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|---|---|
| Molecular Weight |
500.78
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| Exact Mass |
498.992
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| CAS # |
99592-39-9
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| Related CAS # |
Sertaconazole;99592-32-2
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| PubChem CID |
200103
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| Appearance |
White to off-white solid powder
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| Boiling Point |
614.1ºC at 760mmHg
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| Melting Point |
158-160°
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| Flash Point |
325.2ºC
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| LogP |
7.191
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
6
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| Rotatable Bond Count |
6
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| Heavy Atom Count |
31
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| Complexity |
513
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| Defined Atom Stereocenter Count |
0
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| InChi Key |
HAAITRDZHUANGT-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C20H15Cl3N2OS.HNO3/c21-14-4-5-16(18(23)8-14)19(9-25-7-6-24-12-25)26-10-13-11-27-20-15(13)2-1-3-17(20)222-1(3)4/h1-8,11-12,19H,9-10H2(H,2,3,4)
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| Chemical Name |
1-[2-[(7-chloro-1-benzothiophen-3-yl)methoxy]-2-(2,4-dichlorophenyl)ethyl]imidazolenitric acid
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| Synonyms |
Dermofix Ertaczo Zalain Dermoseptic Ginedermofix Mykosert
sertaconazole Zalain
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month Note: Please store this product in a sealed and protected environment, avoid exposure to moisture. |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO : ≥ 100 mg/mL (~199.69 mM)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (4.99 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.5 mg/mL (4.99 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.5 mg/mL (4.99 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 1.9969 mL | 9.9844 mL | 19.9688 mL | |
| 5 mM | 0.3994 mL | 1.9969 mL | 3.9938 mL | |
| 10 mM | 0.1997 mL | 0.9984 mL | 1.9969 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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