Antitrypanosomal agent 15 

Antitrypanosomal agent 15 (compound 26) is an orally active, brain-penetrant, selective inhibitor against Trypanosoma cruzi proteasome, with an _pIC₅₀ of 7.4 and <4 for T. cruzi and human proteasome, respectively. Antitrypanosomal agent 15 has favorable ADME properties and can be used for Chagas disease study^[1].

Antitrypanosomal agent 15 (compound 26) has _pEC₅₀ of 6.1 and 4.4 against intracellular T. cruzi amastigotes and host VERO cells, and has efflux ratio of 1.8 and FaSSIF (the fasted state simulated intestinal fluid solubility) of 339 μM^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Antitrypanosomal agent 15 (compound 26) (50 mg/kg b.i.d for 20 days, p.o.) shows good solubility and permeability, but has no curative towards in chronic mouse model of Chagas disease^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

410.40

C₂₁H₁₉FN₄O₄

2961381-94-0

CNC(C1=C(F)C=CC(NC(C2=NN(C(C=C2)=O)CC3=CC=C(OC)C=C3)=O)=C1)=O

Room temperature in continental US; may vary elsewhere.

Please store the product under the recommended conditions in the Certificate of Analysis.

• [1]. Thomas MG, et al. Structure-Guided Design and Synthesis of a Pyridazinone Series of Trypanosoma cruzi Proteasome Inhibitors. J Med Chem. 2023;66(15):10413-10431.  [Content Brief]