ME1111是一种新型的、具有局部治疗活性的抗真菌药物。
Cas No.:1391758-52-3
Sample solution is provided at 25 µL, 10mM.
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ME1111 is a novel, topically active antifungal agent[1-2]. ME1111 effectively inhibits the growth of pathogenic fungi such as dermatophytes, while reaching infection sites through its strong nail-penetrating ability. ME1111 can be utilized in research related to onychomycosis and other fungal infections[3-4].
In vitro, ME1111 (0.06–32μg/mL) was incubated with K562, HepG2, U937, and A431 cells for 72 hours. ME1111 exhibited half-maximal inhibitory concentrations (IC50) ranging from 33 to 47μg/mL against these four human cell lines[5]. ME1111 (0.004–8μg/mL) was also incubated with Trichophyton rubrum strains (MRL 28661, 28663, 28669, 28674, and 28675) and Trichophyton mentagrophytes strains (MRL 27777, 28313, 28360, 28556, and 28641) for 96 hours. ME1111 significantly inhibited the growth of these dermatophytes, with an average IC50 of 0.5μg/mL[6].
In vivo, ME1111 (10% solution) was topically applied once daily for seven consecutive days in a guinea pig model of dermatophyte infection (lesion area: 2.5cm²). ME1111 demonstrated significantly superior clinical and mycological efficacy compared to both the control group (saline treatment) and the positive control group (8% ciclopirox treatment)[7].
References:
[1] Hui X, Jung EC, Zhu H, et al. Antifungal ME1111 in vitro human onychopharmacokinetics. Drug Dev Ind Pharm. 2017 Jan;43(1):22-29.
[2] Takei-Masuda N, Nagira Y, Kubota-Ishida N, et al. Antidermatophyte activity and PK/PD of ME1111 in a guinea pig model of tinea corporis. J Antibiot (Tokyo). 2024 Aug;77(8):533-539.
[3] Khalfe Y, Rosen T. Future Fungal Fighters in Dermatology: Novel Antifungal Drug Pipeline. J Drugs Dermatol. 2022 May 1;21(5):496-501.
[4] Takahata S, Kubota N, Takei-Masuda N, et al. Mechanism of Action of ME1111, a Novel Antifungal Agent for Topical Treatment of Onychomycosis. Antimicrob Agents Chemother. 2015 Nov 23;60(2):873-80.
[5] Tabata Y, Takei-Masuda N, Kubota N, et al. Characterization of Antifungal Activity and Nail Penetration of ME1111, a New Antifungal Agent for Topical Treatment of Onychomycosis. Antimicrob Agents Chemother. 2015 Dec 7;60(2):1035-9.
[6] Ghannoum M, Chaturvedi V, Diekema D, et al. Multilaboratory Evaluation of In Vitro Antifungal Susceptibility Testing of Dermatophytes for ME1111. J Clin Microbiol. 2016 Mar;54(3):662-5.
[7] Long L, Hager C, Ghannoum M. Evaluation of the Efficacy of ME1111 in the Topical Treatment of Dermatophytosis in a Guinea Pig Model. Antimicrob Agents Chemother. 2016 Mar 25;60(4):2343-5.
ME1111是一种新型的、具有局部治疗活性的抗真菌药物[1-2]。ME1111可有效抑制皮肤癣菌等致病真菌的生长，同时通过良好的指甲穿透性以到达感染部位。ME1111可用于甲癣和相关真菌感染的相关研究[3-4]。
在体外，ME1111（0.06–32μg/mL）孵育K562、HepG2、U937、A431细胞72小时，ME1111细胞对四种人类细胞系的半数抑制浓度（IC50）为33至47μg/mL[5]。ME1111（0.004–8μg/mL）孵育Trichophyton. rubrum（MRL 28661，28663，28669，28674和28675），Trichophyton. mentagrophytes（MRL 27777，28313，28360，28556和28641）96小时，ME1111可显著抑制这些皮肤癣菌的生长，平均IC50为0.5μg/mL[6]。
在体内，ME1111（10%溶液）每天一次局部用药连续七天，处理豚鼠背部皮肤癣菌感染模型（伤口面积为2.5cm2）。ME1111在临床和真菌学疗效上均显著优于对照组（生理盐水处理）和阳性对照组（8%环吡酮处理）[7]。
| Cell experiment [1]: | |
Cell lines | Human cell lines K562, HepG2, U937, A431 (leukemia, liver tumor, lymphoma, and skin origin, respectively) |
Preparation Method | The human cell lines were cultured in growth medium under 5% CO₂ at 37°C. After 24 hours, ME1111 (at concentrations ranging from 0.06 to 32μg/mL) was added, followed by a 72-hour incubation. |
Reaction Conditions | 0.06 to 32μg/mL; 72 hours. |
Applications | ME1111 showed minimal inhibition of human cell proliferation, with IC₅₀ values of 47, 37, 33, and 40μg/mL for K562, HepG2, U937, and A431 cells, respectively. The selectivity for inhibiting Trichophyton spp. (MIC₉₀=0.5μg/mL) over human cells was approximately 60-fold higher, indicating low host cell toxicity and a favorable therapeutic index. |
| Animal experiment [2]: | |
Animal models | Male albino guinea pigs (Harlan-Sprague-Dawley) |
Preparation Method | Guinea pigs were infected by topically applying a conidial suspension containing 1x10⁷ T. mentagrophytes conidia onto abraded skin on their backs. 10% ME1111 solution treatment began 72 hours post-infection. |
Dosage form | 10% ME1111 solution; Topical application; Once daily for seven consecutive days. |
Applications | ME1111 treatment led to significant clinical and mycological efficacy against dermatophytosis. The clinical efficacy of ME1111 was superior to that of 8% ciclopirox. |
References: | |
| Cas No. | 1391758-52-3 | SDF | |
| 分子式 | C12H14N2O | 分子量 | 202.25 |
| 溶解度 | DMSO : 100 mg/mL (494.44 mM; Need ultrasonic) | 储存条件 | Store at -20°C |
| General tips | 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；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。 储备液的保存方式和期限：-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 4.9444 mL | 24.7219 mL | 49.4438 mL |
| 5 mM | 988.9 μL | 4.9444 mL | 9.8888 mL |
| 10 mM | 494.4 μL | 2.4722 mL | 4.9444 mL |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
3. 以上所有助溶剂都可在 GlpBio 网站选购。
Quality Control & SDS
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- Purity: >99.50% Appearance: A solid
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