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Antitrypanosomal Agent 15 (Compound 26) is an orally active, brain-penetrant, selective inhibitor of the Trypanosoma cruzi proteasome, exhibiting a pIC50 of 7.4 for T. cruzi and <4 for the human proteasome. It possesses favorable ADME properties, rendering it useful for the study of Chagas disease [1].
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| 5 mg | Inquiry | Inquiry | Inquiry | |
| 50 mg | Inquiry | Inquiry | Inquiry |
| Description | Antitrypanosomal Agent 15 (Compound 26) is an orally active, brain-penetrant, selective inhibitor of the Trypanosoma cruzi proteasome, exhibiting a pIC50 of 7.4 for T. cruzi and <4 for the human proteasome. It possesses favorable ADME properties, rendering it useful for the study of Chagas disease [1]. |
| In vitro | Antitrypanosomal agent 15 (compound 26) demonstrated pEC50 values of 6.1 against T. cruzi amastigotes and 4.4 for host VERO cells, with a selectivity index of 1.8, and a solubility in FaSSIF (fasted state simulated intestinal fluid) of 339 μM [1]. |
| In vivo | Antitrypanosomal agent 15 (compound 26), administered orally at 50 mg/kg twice daily for 20 days, demonstrated good solubility and permeability but showed no efficacy in a chronic Chagas disease mouse model [1]. |
| Molecular Weight | 410.4 |
| Formula | C21H19FN4O4 |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature. |
Dissolve 2 mg of the compound in 100 μL DMSO
to obtain a stock solution at a concentration of 20 mg/mL . If the required concentration exceeds the compound's known solubility, please contact us for technical support before proceeding.
1) Add 100 μL of the DMSO
stock solution to 400 μL PEG300
and mix thoroughly until the solution becomes clear.
2) Add 50 μL Tween 80 and mix well until fully clarified.
3) Add 450 μL Saline,PBS or ddH2O
and mix thoroughly until a homogeneous solution is obtained.
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