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Antitrypanosomal agent 15

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Catalog No. T79316

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].

Antitrypanosomal agent 15

Antitrypanosomal agent 15

😃Good
Catalog No. T79316
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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Product Introduction

Bioactivity
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].
Chemical Properties
Molecular Weight410.4
FormulaC21H19FN4O4
Storage & Solubility Information
StorageShipping with blue ice.

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TargetMol | Animal experimentsFor example, your dosage is 10 mg/kg Each animal weighs 20 g, and the dosage volume is 100 μL . TargetMol | Animal experiments A total of 10 animals were administered, and the formula you used is 5% TargetMol | reagent DMSO+30% PEG300+5% Tween 80+60% ddH2O. So your working solution concentration is 2 mg/mL。
Mother liquor preparation method: 2 mg of drug dissolved in 50 μL DMSOTargetMol | reagent (mother liquor concentration of 40 mg/mL), if you need to configure a concentration that exceeds the solubility of the product, please contact us first.
Preparation method for in vivo formula: Take 50 μL DMSOTargetMol | reagent main solution, add 300 μLPEG300TargetMol | reagent mix well and clarify, then add 50 more μL Tween 80, mix well and clarify, then add 600 more μLddH2OTargetMol | reagent mix well and clarify
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