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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].
Pack Size | Price | Availability | Quantity |
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5 mg | Inquiry | Backorder | |
50 mg | Inquiry | Backorder |
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 | Shipping with blue ice. |
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