| 产品介绍 |
T-2307 是一种芳基脒,在体外和体内具有抗真菌活性。T-2307 具有广谱抗菌活性,包括念珠菌属 (Candida, MIC 为 0.00025 至 0.0078 μg/mL)、新型隐球菌属 (Cryptococcus neoformans,MIC 为 0.0039-0.0625 μg/mL) 和曲霉属 (Aspergillus;MIC 为 0.0156-4 μg/mL)。
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| 生物活性 |
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) .
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| 体外研究 |
T-2307 exhibits potent activity against fluconazole-resistant and fluconazole-susceptible-dose-dependent Candida albicans strains as well as against azole-susceptible strains.
T-2307 shows efficacy in a murine model of candida glabrata infection despite in vitro trailing growth phenomena.
西域 has not independently confirmed the accuracy of these methods. They are for reference only.
Cell Viability Assay
| 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.
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体内研究 (In Vivo) |
In mouse models of disseminated candidiasis, cryptococcosis, and aspergillosis, the ED50 of T-2307 were 0.00755, 0.117, and 0.391 mg/kg, respectively.
西域 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. |
| 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 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 significantly 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 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 ED50s of T-2307 were 0.391 mg/kg. |
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| 体内研究 |
In mouse models of disseminated candidiasis, cryptococcosis, and aspergillosis, the ED50 of T-2307 were 0.00755, 0.117, and 0.391 mg/kg, respectively.
西域 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. |
| 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 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 significantly 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 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 ED50s of T-2307 were 0.391 mg/kg. |
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| 体内研究 |
In mouse models of disseminated candidiasis, cryptococcosis, and aspergillosis, the ED50 of T-2307 were 0.00755, 0.117, and 0.391 mg/kg, respectively.
西域 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. |
| 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 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 significantly 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 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 ED50s of T-2307 were 0.391 mg/kg. |
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| 性状 | Solid |
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| 溶解性数据 |
In Vitro:
DMSO : 50 mg/mL (114.26 mM; ultrasonic and adjust pH to 3 with HCl)
配制储备液
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浓度
溶剂体积
质量
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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 |
*
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, 6 months; -20°C, 1 month。-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。
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| 运输条件 |
Room temperature in continental US; may vary elsewhere.
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| 储存方式 |
| Powder |
-20°C |
3 years |
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4°C |
2 years |
| In solvent |
-80°C |
6 months |
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-20°C |
1 month |
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| 参考文献 | |
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