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Tolnaftate/托萘酯 ≥99%

货号:A357832 同义名: NP-27; NSC 233648

Tolnaftate是一种合成的硫代氨基甲酸酯类抗真菌药。

Tolnaftate/托萘酯 化学结构 CAS号:2398-96-1
Tolnaftate/托萘酯 化学结构
CAS号:2398-96-1
Tolnaftate/托萘酯 3D分子结构
CAS号:2398-96-1
Tolnaftate/托萘酯 化学结构 CAS号:2398-96-1
规格 价格 库存 数量
50μL*10mM(DMSO) ¥99随货¥69 现货 - +
100μL*10mM(DMSO) ¥109随货¥79 现货 - +
250μL*10mM(DMSO) ¥119随货¥89 现货 - +
500μL*10mM(DMSO) ¥159随货¥119 现货 - +
10mM*1mL(DMSO) ¥222 现货 - +
500mg ¥126 现货 - +
1g ¥202 现货 - +
5g ¥504 现货 - +
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Tolnaftate/托萘酯 纯度/质量文件 产品仅供科研

货号:A357832 标准纯度: ≥99%
批次查询: 批次纯度: 99.25%

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Tolnaftate/托萘酯 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].

Tolnaftate/托萘酯 细胞实验

Cell Line
Concentration Treated Time Description References
Trichophyton rubrum 0.01-0.20 µg/ml Evaluate the antifungal activity of ME1401 against Trichophyton rubrum, showing that ME1401 was more active than four reference drugs (including clotrimazole), and all strains were inhibited by 0.20 µg/ml of ME1401. Antimicrob Agents Chemother. 1986 Nov;30(5):705-12.
Trichophyton mentagrophytes 0.025-0.39 µg/ml Evaluate the antifungal activity of ME1401 against Trichophyton mentagrophytes, showing that ME1401 was comparable to clotrimazole for susceptible strains but much stronger than tolnaftate, miconazole, haloprogin, and ciclopirox olamine. Antimicrob Agents Chemother. 1986 Nov;30(5):705-12.
Huh7.5.1 cells 10 µM 3 days To evaluate the effect of Tolnaftate on the clinical prognostic liver signature (PLS), results showed that Tolnaftate significantly reversed the poor-prognosis status of PLS Nat Commun. 2021 Sep 17;12(1):5525.

Tolnaftate/托萘酯 动物实验

Species
Animal Model
Administration Dosage Frequency Description References
New Zealand albino rabbits Fungal keratitis model Ocular administration 50 µg Single dose, duration of 24 hours To evaluate the antifungal efficacy of Tolnaftate in the eye, results showed that PSR1 sustained antifungal activity up to 24 hours. Drug Deliv. 2022 Dec;29(1):2162-2176

Tolnaftate/托萘酯 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 <<

Tolnaftate/托萘酯 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

Tolnaftate/托萘酯 实验方案

计算器
存储液制备 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

Tolnaftate/托萘酯 技术信息

CAS号2398-96-1
分子式C19H17NOS
分子量 307.41
SMILES Code S=C(OC1=CC=C2C=CC=CC2=C1)N(C)C3=CC=CC(C)=C3
MDL No. MFCD00056611
别名 NP-27; NSC 233648; Tolnaftate, Tinactin, Tinaderm, Aftate, NP-27, NP 27, NP27; SCH 10144
运输蓝冰
InChI Key FUSNMLFNXJSCDI-UHFFFAOYSA-N
Pubchem ID 5510
存储条件

In solvent -20°C: 3-6个月 -80°C: 12个月

Pure form Sealed in dry, 2-8°C

溶解方案

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

请根据您的动物给药指南选择适当的溶解方案。
以下溶解方案都请先按照体外实验的方式配制澄清的储备液,再依次添加助溶剂:
——为保证实验结果的可靠性,澄清的储备液可以根据储存条件,适当保存;体内实验的工作液,建议现用现配,当天使用; 以下溶剂前显示的百分比是指该溶剂在终溶液中的体积占比;如在配制过程中出现沉淀、析出现象,可以通过加热和/或超声的方式助溶
方案 一
请依序添加每种溶剂:10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 3.25 mg/mL (10.57 mM); 澄清溶液
此方案可获得 ≥ 3.25 mg/mL(饱和度未知)的澄清溶液。
以 1 mL 工作液为例,取 100 μL 32.5 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中,混合均匀;再向上述体系中加入 50 μL Tween-80,混合均匀;然后再继续加入 450 μL 生理盐水 定容至 1 mL。
生理盐水的配制:将 0.9 g 氯化钠,溶解于 ddH₂O 并定容至 100 mL,可以得到澄清透明的生理盐水溶液。
方案 二
请依序添加每种溶剂:10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 3.25 mg/mL (10.57 mM); 澄清溶液
此方案可获得 ≥ 3.25 mg/mL(饱和度未知)的澄清溶液。
以 1 mL 工作液为例,取 100 μL 32.5 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液 中,混合均匀。
2 g SBE-β-CD(磺丁基醚 β-环糊精)粉末定容于 10 mL 的生理盐水中,完全溶解至澄清透明。
方案 三
请依序添加每种溶剂:10% DMSO 90% Corn Oil
Solubility: ≥ 3.25 mg/mL (10.57 mM); 澄清溶液
此方案可获得 ≥ 3.25 mg/mL(饱和度未知)的澄清溶液,此方案实验周期在半个月以上的动物实验酌情使用。
以 1 mL 工作液为例,取 100 μL 32.5 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中,混合均匀。
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