ME1111 |
Catalog No.GC62398
One-Click Copy Product Info
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ME1111 is a novel, topically active antifungal agent.
Products are for research use only. Not for human use. We do not sell to patients.
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.
| 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 | |
| Formula | C12H14N2O | M.Wt | 202.25 |
| Solubility | DMSO : 100 mg/mL (494.44 mM; Need ultrasonic) | Storage | Store at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
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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 |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
g
μL
Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)
Calculation results:
Working concentration: mg/ml;
Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid 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 master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL saline, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
- View current batch:
- Purity: >99.50% Appearance: A solid
- COA (Certificate of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 34 reference(s) in Google Scholar.)