[CAS NO. 873546-31-7] T-2307
PRODUCTS SPECIFICATIONS [873546-31-7]
DESCRIPTION [873546-31-7]
Overview
| MDL | - |
|---|---|
| Molecular Weight | 437.58 |
| Molecular Formula | C25H35N5O2 |
| SMILES | N=C(C1=CC=C(OCCCN2CCC(CCCOC3=CC=C(C(N)=N)C=C3)CC2)C=C1)N |
Summary
T-2307, an arylamidine, has antifungal activities in vitro and in vivo. T-2307 exhibits broad-spectrum activity against clinically significant pathogens, including Candida species (MIC range, 0.00025 to 0.0078 μg/ml), Cryptococcus neoformans (MIC range, 0.0039 to 0.0625 μg/ml), and Aspergillus species (MIC range, 0.0156 to 4 μg/mL) [1] .
In Vitro
T-2307 exhibits potent activity against fluconazole-resistant and fluconazole-susceptible-dose-dependent
Candida albicans
strains as well as against azole-susceptible strains
[1]
.
T-2307 shows efficacy in a murine model of
candida glabrata
infection despite in vitro trailing growth phenomena
[2]
.
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Cell Viability Assay [2]
| Cell Line: | C. glabrata ATCC 90030 |
| Concentration: | 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 Time: | 24 and 48 hours |
| Result: |
C. glabrata
exhibited significant trailing growth at concentrations between 0.0039 and 0.125 μg/mL at 48 h.
The trailing growth of C. glabrata at 24 h of incubation was similar to that at 48 h. |
In Vivo
In mouse models of disseminated candidiasis, cryptococcosis, and aspergillosis, the ED 50 of T-2307 were 0.00755, 0.117, and 0.391 mg/kg, respectively [1] .
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
| Animal Model: | 4-week-old specific-pathogen-free ICR strain male mice bearing systemic infections with Candida albicans , Cryptococcus neoformans , and Aspergillus fumigatus [1] . |
| Dosage: | 0.001, 0.1, 1 mg/kg |
| Administration: | Subcutaneously administered; once a day for 7 days, beginning at 2 h after the infection. |
| Result: |
In the systemic infection caused by
Candida albicans
, all the control mice died by day 6. Mortality was significantly 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 ED
50
s 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 significantly delayed in mice administered T-2307 at a dose of 0.1 mg/kg compared with that in the control mice. The calculated ED 50 s 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 significantly delayed in mice that were administered T-2307 at a dose of 1 mg/kg compared with that in the control mice. The calculated ED 50 s of T-2307 were 0.391 mg/kg. |
Appearance
Solid
Shipping
Room temperature in continental US; may vary elsewhere.
Storage
| Powder | -20°C | 3 years |
|---|---|---|
| 4°C | 2 years | |
| In solvent | -80°C | 6 months |
| -20°C | 1 month |
Solvent & Solubility
DMSO : 50 mg/mL ( 114.26 mM ; ultrasonic and adjust pH to 3 with HCl)
Stock Solutions
| Concentration Solvent Mass | 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 |
References
- [1] Junichi Mitsuyama, et al. In vitro and in vivo antifungal activities of T-2307, a novel arylamidine. Antimicrob Agents Chemother. 2008 Apr;52(4):1318-24.
- [2] Eio Yamada, et al. T-2307 shows efficacy in a murine model of Candida glabrata infection despite in vitro trailing growth phenomena. Antimicrob Agents Chemother. 2010 Sep;54(9):3630-4.