| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| Other Sizes |
| Targets |
Fungal targets (PKA pathway via Tpk2 catabolic subunit and its binding target Sfl1).
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|---|---|
| ln Vitro |
In a dose-dependent manner, mutanocyclin (8, 16, 32 µg/mL, 24, 36 hours) suppresses the filamentation of Candida albicans [1].
In C. albicans cells, mutanocyclin (32 µg/mL) decreases the mRNA expression of HWP1, ECE1, FLO8, and TEC1 [1]. The PKA catabolic component Tpk2 and its preferred binding target Sfl1 are regulated by mutanocyclin [1]. Mutanocyclin potently inhibits Candida albicans filamentation, a key virulence factor for this opportunistic fungal pathogen. It reduces the mRNA expression of filamentation-associated genes including HWP1, ECE1, FLO8, and TEC1. In a dose-dependent manner at concentrations of 8-32 ug/mL, mutanocyclin suppresses hyphal formation. It functions by regulating the PKA catabolic subunit Tpk2 and its binding target Sfl1. |
| ln Vivo |
The yeast form of C is inhibited by mutanocyclin (32 µg/mL; infected mouse tongue for 24 hours). albicans in a model of tongue infection in ex vivo mice [1]. In 48 hours, mutanocyclin (6.4, 12.8, 25.6 µg/mL) reduces the pathogenicity of C. Candida in the G. model of mellonella infection [1].
In ex vivo experiments using isolated mouse tissue, mutanocyclin inhibits the yeast-to-hypha transition of C. albicans. At concentrations of 8, 16, and 32 ug/mL, the compound suppresses yeast forms. Additionally, it demonstrates the ability to inhibit oral biofilm formation and modulate fungal virulence in a human saliva-derived in vitro biofilm model, although potency is lower compared to its acylated congener reutericyclin A. |
| Enzyme Assay |
Assay: Candida albicans filamentation inhibition assay. Protocol: C. albicans cells (SC5314 strain, 1×10⁴ cells) are incubated in BHI-sucrose medium with mutanocyclin at concentrations of 8, 16, and 32 ug/mL or DMSO control at 30degC for 24-36 hours. Cells are then examined microscopically to quantify the percentage of filamentous cells versus yeast-form cells. IC50 for filamentation inhibition is determined from dose-response curves.
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| Cell Assay |
Cells: C. albicans (SC5314 strain). Protocol: For gene expression analysis, C. albicans cells are treated with mutanocyclin at 32 ug/mL for 4-6 hours. Total RNA is extracted and subjected to qRT-PCR to measure mRNA levels of HWP1, ECE1, FLO8, and TEC1, normalized to ACT1 (actin) as an internal control. For biofilm assays, C. albicans is cultured in 96-well plates with mutanocyclin (0-100 ug/mL), and biofilm formation is quantified by crystal violet staining.
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| Animal Protocol |
Animal Model: Ex vivo mouse tissue model (isolated mouse tissue). Protocol: Mouse tissue (e.g., tongue or vaginal mucosa explants) is inoculated with C. albicans (10⁶ cells) and incubated with mutanocyclin at 8-32 ug/mL for 24-48 hours. Tissues are then homogenized, and fungal burden is quantified by CFU plating on Sabouraud dextrose agar. Filamentation is assessed microscopically in tissue sections stained with fungal-specific dyes (e.g., calcofluor white).
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| ADME/Pharmacokinetics |
No specific PK data found for mutanocyclin; please refer to general properties of tetramic acid secondary metabolites: These compounds are typically small (MW ~200-400), moderately lipophilic (logP 2-3), and may exhibit short plasma half-lives due to rapid metabolism. Oral bioavailability is often low, necessitating parenteral administration for in vivo efficacy studies. High plasma protein binding is common.
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| Toxicity/Toxicokinetics |
No specific data found; mutanocyclin is an investigational compound. As a natural product antifungal agent, it has been studied in ex vivo mouse models at concentrations up to 32 ug/mL with no apparent toxicity to host tissues reported. However, comprehensive toxicological profiling (MTD, organ toxicity, genotoxicity) has not been published. Higher potency acylated congeners may exhibit distinct toxicity profiles.
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| References | |
| Additional Infomation |
Mutanocyclin are enols and enones.
Mutanocyclin was first characterized in 2019 as a metabolite of Streptococcus mutans that suppresses filamentous growth of Candida albicans. This cross-kingdom interaction represents an ecological mechanism by which S. mutans competes with C. albicans in the oral cavity. Mutanocyclin exhibits dramatically lower potency in inhibiting oral biofilm formation compared to its acylated congener reutericyclin A. It is an investigational compound not approved for human use. |
| Molecular Formula |
C10H15NO3
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|---|---|
| Molecular Weight |
197.231
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| Exact Mass |
197.105
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| CAS # |
875455-92-8
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| PubChem CID |
54683942
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| Appearance |
White to off-white solid powder
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| LogP |
1.2
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| Hydrogen Bond Donor Count |
2
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| Hydrogen Bond Acceptor Count |
3
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| Rotatable Bond Count |
3
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| Heavy Atom Count |
14
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| Complexity |
305
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| Defined Atom Stereocenter Count |
1
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| SMILES |
CC(CC1NC(O)=C(C(=O)C)C1=O)C
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| InChi Key |
SHHAXAUQMPMPRV-SSDOTTSWSA-N
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| InChi Code |
InChI=1S/C10H15NO3/c1-5(2)4-7-9(13)8(6(3)12)10(14)11-7/h5,7,13H,4H2,1-3H3,(H,11,14)/t7-/m1/s1
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| Chemical Name |
(2R)-4-acetyl-3-hydroxy-2-(2-methylpropyl)-1,2-dihydropyrrol-5-one
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
May dissolve in DMSO (in most cases), if not, try other solvents such as H2O, Ethanol, or DMF with a minute amount of products to avoid loss of samples
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| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 5.0702 mL | 25.3511 mL | 50.7022 mL | |
| 5 mM | 1.0140 mL | 5.0702 mL | 10.1404 mL | |
| 10 mM | 0.5070 mL | 2.5351 mL | 5.0702 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution 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 stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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