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Tolnaftate

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Chemical Structure| 2398-96-1 同义名 : NP-27;NSC 233648;Tolnaftate, Tinactin, Tinaderm, Aftate, NP-27, NP 27, NP27;SCH 10144
CAS号 : 2398-96-1
货号 : A357832
分子式 : C19H17NOS
纯度 : 98%
分子量 : 307.409
MDL号 : MFCD00056611
存储条件:

粉末 Sealed in dry,2-8°C

液体 -20°C:3-6个月-80°C:12个月

溶解度 :

DMSO: 50 mg/mL(162.65 mM),配合低频超声助溶,注意:DMSO长时间开封后,会吸水并导致溶解能力下降,请避免使用长期开封的DMSO

动物实验配方:
生物活性
描述 Tolnaftate, is a topical antifungal agent described to be effective in the treatment of otomycosis[3]. Cells grown in the presence of tolnaftate (at the IC50) showed a reduced content of total phospholipids and sterols whereas there was an increase in total RNA content. The activity of membrane-bound enzymes did not change on treatment with tolnaftate (10 x MIC) whereas an increase in the leakage of intracellular 32P was observed. Activity of phosphodiesterase decreased and 5'-nucleotidase increased in tolnaftate-resistant cells[4]. In vitro skin penetration studies revealed that after application of 1% (w/w) tolnaftate solution in polyethylene glycol 400 for 24 hours, the mean amount of tolnaftate penetrating into the epidermis and dermis was 2.60 +/- 0.28 mg/cm2 and 0.92 +/- 0.12 mg/cm2, respectively[5]. The thiocarbamate antimycotics tolnaftate and tolciclate blocked sterol biosynthesis in fungal cells and cell extracts, with accumulation of squalene. The biochemical action of tolnaftate and tolciclate is thus similar to that of the allylamine antimycotics naftifine and terbinafine[6].
临床研究
NCT号 适应症或疾病 临床期 招募状态 预计完成时间 地点
NCT02413840 COPD Anxiety ... 展开 >> Depression 收起 << Not Applicable Unknown - China ... 展开 >> Beijing institute of respiratory diseases Recruiting Beijing, China Contact: Ting Yang    8613651380809 收起 <<
NCT02187679 Tourette Syndrome ... 展开 >> Chronic Vocal Tic 收起 << Not Applicable Unknown - United States, Michigan ... 展开 >> Detroit Clinical Research Center Recruiting Farmington Hills, Michigan, United States, 48334 Contact: Candice Shallal, BS    248-716-7009 ext 190    candice.shallal@dcrc.us    Principal Investigator: Edward Dabrowski, MD 收起 <<
NCT00401908 - Withdrawn - United States, New York ... 展开 >> Maimonides Medical Center Brooklyn, New York, United States, 11219 收起 <<
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

3.25mL

0.65mL

0.33mL

16.26mL

3.25mL

1.63mL

32.53mL

6.51mL

3.25mL

参考文献

[1]Georgopapadakou NH, Bertasso A. Effects of squalene epoxidase inhibitors on Candida albicans. Antimicrob Agents Chemother. 1992 Aug;36(8):1779-81.

[2]Ryder NS, Frank I, et al. Ergosterol biosynthesis inhibition by the thiocarbamate antifungal agents tolnaftate and tolciclate. Antimicrob Agents Chemother. 1986 May;29(5):858-60.

[3]Jimenez-Garcia L, Celis-Aguilar E, Díaz-Pavón G, et al. Efficacy of topical clotrimazole vs. topical tolnaftate in the treatment of otomycosis. A randomized controlled clinical trial [published online ahead of print, 2019 Feb 18]. Braz J Otorhinolaryngol. 2019;S1808-8694(18)30274-X

[4]Gupta MP, Kapur N, Bala I, Khuller GK. Studies on the mode of action of tolnaftate in Microsporum gypseum. J Med Vet Mycol. 1991;29(1):45‐52

[5]Kezutyte T, Kornysova O, Maruska A, Briedis V. Assay of tolnaftate in human skin samples after in vitro penetration studies using high performance liquid chromatography. Acta Pol Pharm. 2010;67(4):327‐334

[6]Ryder NS, Frank I, Dupont MC. Ergosterol biosynthesis inhibition by the thiocarbamate antifungal agents tolnaftate and tolciclate. Antimicrob Agents Chemother. 1986;29(5):858‐860