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
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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