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T. cruzi bc1 inhibitor compound 4

Chemical Structure : T. cruzi bc1 inhibitor compound 4

CAS No.:

T. cruzi bc1 inhibitor compound 4

Catalog No.: PC-21591Not For Human Use, Lab Use Only.

T. cruzi bc1 inhibitor compound 4 is a highly selective and efficacious T. cruzi cytochrome b inhibitor with IC50 of 6 nM, exhibits potent activity against intracellular amastigotes with EC50 of 0.08 uM.

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Purity & Documentation Purity: >98% (HPLC)

Biological Activity

T. cruzi bc1 inhibitor compound 4 is a highly selective and efficacious T. cruzi cytochrome b inhibitor with IC50 of 6 nM, exhibits potent activity against intracellular amastigotes with EC50 of 0.08 uM.
T. cruzi bc1 inhibitor compound 4 displays no apparent cytotoxicity against either Vero host cells or uninfected HepG2 cells (pEC50 < 4.5).
T. cruzi bc1 inhibitor compound 4 does not inhibit human complex III, does not reduces the calcium loading capacity (CLC) of isolated rat liver mitochondria at 200 uM.
T. cruzi bc1 inhibitor compound 4 (50, 30, or 10 mg/kg bid) exhibits full efficacy against experimental chronic Chagas disease when dosed orally for 5 days in combination with benznidazole (BNZ).
T. cruzi bc1 inhibitor 4 inhibits the Qi active site of T. cruzi cytochrome b, part of the cytochrome bc1 complex of the electron transport chain.

Physicochemical Properties

M.Wt 298.35
Formula C16H18N4O2
Appearance Solid
CAS No.
Storage
Solide Powder
-20°C 12 Months; 4°C 6 Months
In Solvent
-80°C 6 Months; -20°C 6 Months
Shipping
Solubility

10 mM in DMSO

Chemical Name/SMILES

5-(2,4-Dimethoxyphenyl)-4,6-dimethyl-7H-pyrrolo[2,3-d]pyrimidin-2-amine

References

1. Silvia González, et al. Sci Transl Med. 2023 Dec 13;15(726):eadg8105.

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