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1、Hotline: 400-820-3792Inhibitors Agonists Screening Librarieswww.MedChemETerconazoleCat. No.: HY-B1790CAS No.: 67915-31-5Synonyms: R42470分式: CHClNO分量: 532.46作靶点: Fungal作通路: Anti-infection储存式: Powder -20C 3 years4C 2 yearsIn solvent -80C 6 months-20C 1 month溶解性数据体外实验 DMSO : 30 mg/mL (56.34 mM)* means
2、soluble, but saturation unknown.Mass Solvent1 mg 5 mg 10 mg Concentration制备储备液1 mM 1.8781 mL 9.3904 mL 18.7808 mL5 mM 0.3756 mL 1.8781 mL 3.7562 mL10 mM 0.1878 mL 0.9390 mL 1.8781 mL请根据产品在不同溶剂中的溶解度,选择合适的溶剂配制储备液,并请注意储备液的保存式和期限。BIOLOGICAL ACTIVITY物活性 Terconazole于治疗道酵母感染的谱抗真药物。体外研究Terconazole inhibits
3、the growth of Candida albicans ATCC 44859 in a concentration-related manner, but withmodest effects noted at levels from 0.1 to 10 M when the yeast is grown on media favoring the cell form.The inhibitory potency of terconazole on yeast cell viability varies with the strain and species of Candida1/2
4、Master of Small Molecules 您边的抑制剂师www.MedChemEtested. The susceptibility of C. albicans ATCC 44859 to terconazole is markedly enhanced when the yeast isgrown on Eagle minimum essential medium, which favors mycelium formation. There is a progression ofchanges, from loss of mycelia formation at 0.1 M t
5、erconazole through complete necrosis at 100 M 1.Terconazole blocks the morphogenetic transformation from the yeast into the filamentous form atconcentrations of 0.008 to 0.05 microgram/mL 2.体内研究 A 3-day once-daily intravaginal application of terconazole 0.8% is usually sufficient to provide a functi
6、onaltherapeutic period of 7 days because of prolonged high biologically active antifungal levels in the vagina. Noside effects are observed at any concentration of terconazole 2.PROTOCOLAnimal Rats: The rats are infected intravaginally with C. albicans. They are treated topically twice daily for 3 d
7、ays,Administration 2 starting 24 hours after infection with a volume of 0.2 mL of various concentrations of terconazole (0.125%,0.25%, 0.4%, 0.5%, 1%, 2%), miconazole, clotrimazole, econazole, nystatin, or amphotericin B 2.MCE has not independently confirmed the accuracy of these methods. They are f
8、or reference only.REFERENCES1. Tolman EL, et al. Anticandidal activities of terconazole, a broad-spectrum antimycotic. Antimicrob Agents Chemother. 1986Jun;29(6):986-91.2. Van Cutsem J, et al. The in vitro activity of terconazole against yeasts: its topical long-acting therapeutic efficacy in experimental vaginalcandidiasis in rats. Am J Obstet Gynecol. 1991 Oct;165(4 Pt 2):1200-6.McePdfHeightCaution: Product has not been fully validated for medical applicat
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