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| Targets |
Mitochondrial respiratory chain complexes in fungal cells.
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| ln Vitro |
T-2307 shows strong efficacy against azole-sensitive strains of Candida albicans as well as strains that are dose-dependently susceptible to fluconazole[1]. In spite of in vitro lagging growth abnormalities, T-2307 demonstrates effectiveness in a murine model of candida glabrata infection[2].
T-2307 exhibits potent activity against a wide range of fungi, including Candida species (MICs: 0.00025-0.0078 microg/mL), Cryptococcus neoformans (MICs: 0.0039-0.0625 microg/mL), and Aspergillus species (MICs: 0.0156-4 microg/mL). It is also effective against fluconazole-resistant and azole-susceptible Candida albicans strains. |
| ln Vivo |
T-2307's ED50 values in mice models of aspergillosis, cryptococcosis, and disseminated candidiasis were 0.00755, 0.117, and 0.391 mg/kg, correspondingly[1].
In mouse models of disseminated candidiasis, cryptococcosis, and aspergillosis, T-2307 demonstrated potent in vivo efficacy with ED50 values of 0.00755, 0.117, and 0.391 mg/kg, respectively. This confirms its excellent in vivo activity against systemic fungal infections. |
| Enzyme Assay |
The antifungal activity is assessed by determining the Minimum Inhibitory Concentration (MIC) using the broth microdilution method according to CLSI guidelines. A panel of fungal strains, including drug-resistant isolates, is tested with serial dilutions of T-2307.
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| Cell Assay |
Cell Viability Assay[2]
Cell Types: C. glabrata ATCC 90030 Tested Concentrations: 0.000125, 0.00025, 0.0005, 0.001, 0.002, 0.0039, 0.0078, 0.0156, 0.0313, 0.0625, 0.125 μg/mL Incubation Duration: 24 and 48 hrs (hours) Experimental Results: C. glabrata demonstrated significant trailing growth at concentrations between 0.0039 and 0.125 μg/mL at 48 h. The trailing The growth of C. glabrata at 24 h of incubation was similar to that at 48 h. Cell viability assays are performed against fungal cells. The minimum fungicidal concentration (MFC) is determined by subculturing from wells with no visible growth onto agar plates to assess the compound's ability to kill, rather than just inhibit, the fungal cells. |
| Animal Protocol |
Animal/Disease Models: 4weeks old specific-pathogen-free ICR strain male mice bearing systemic infections with Candida albicans, Cryptococcus neoformans, and Aspergillus fumigatus[1].
Doses: 0.001, 0.1, 1 mg/kg Route of Administration: subcutaneously (sc) administered; one time/day for 7 days, beginning at 2 h after the infection. Experimental Results: In the systemic infection caused by Candida albicans, all the control mice died by day 6. Mortality was Dramatically delayed in mice that were administered T-2307 at a dose of 0.01 mg/kg compared with that in the control mice. The calculated ED50s of T-2307were 0.00755 mg/kg. In the systemic infection caused by Cryptococcus neoformans, all the control mice died by day 9. Mortality was Dramatically delayed in mice administered T-2307 at a dose of 0.1 mg/kg compared with that in the control mice. The calculated ED50s of T-2307 were 0.117 mg/kg. In the systemic infection caused by Aspergillus fumigatus, all the control mice died by day 6. Mortality was Dramatically delayed i Animal Model: Mouse models of disseminated candidiasis, cryptococcosis, and aspergillosis. Dosage: 0.001, 0.1, 1 mg/kg. Administration: Subcutaneous injection. Endpoints: ED50 values determined by survival or fungal burden in organs. |
| ADME/Pharmacokinetics |
Physicochemical properties: Molecular Weight = 437.58, Molecular Formula = C25H35N5O2. Solubility: DMSO : 50 mg/mL (114.26 mM; adjust pH to 3 with HCl). Storage: Powder -20degC for 3 years; In solvent -80degC for 6 months.
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| References |
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| Additional Infomation |
See also: T-2307 (notes moved to).
T-2307 (CAS#: 873546-31-7) is a promising antifungal agent with a novel mechanism of action targeting mitochondrial function. Its potent activity against azole- and echinocandin-resistant strains makes it a valuable candidate for treating difficult-to-manage fungal infections. It is a research compound and is not yet approved for clinical use. |
| Molecular Formula |
C25H35N5O2
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|---|---|
| Molecular Weight |
437.58
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| Exact Mass |
437.279
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| CAS # |
873546-31-7
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| PubChem CID |
9803135
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| Appearance |
Off-white to light brown solid powder
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| LogP |
5.132
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| Hydrogen Bond Donor Count |
4
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| Hydrogen Bond Acceptor Count |
5
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| Rotatable Bond Count |
12
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| Heavy Atom Count |
32
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| Complexity |
563
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| Defined Atom Stereocenter Count |
0
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| InChi Key |
KUNDLEJVAIBADY-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C25H35N5O2/c26-24(27)20-4-8-22(9-5-20)31-17-1-3-19-12-15-30(16-13-19)14-2-18-32-23-10-6-21(7-11-23)25(28)29/h4-11,19H,1-3,12-18H2,(H3,26,27)(H3,28,29)
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| Chemical Name |
4-[3-[1-[3-(4-carbamimidoylphenoxy)propyl]piperidin-4-yl]propoxy]benzenecarboximidamide
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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) |
DMSO : 50 mg/mL (114.26 mM
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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 | 2.2853 mL | 11.4265 mL | 22.8530 mL | |
| 5 mM | 0.4571 mL | 2.2853 mL | 4.5706 mL | |
| 10 mM | 0.2285 mL | 1.1426 mL | 2.2853 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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