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EDI048

Chemical Structure : EDI048

CAS No.: 2767264-57-1

EDI048 (EDI-048)

Catalog No.: PC-23131Not For Human Use, Lab Use Only.

EDI048 (EDI-048) is a specific, ATP-competitive, gastrointestinal-targeted Cryptosporidium PI(4)K (CpPI(4)K) inhibitor with IC50 of 4 nM, >300-fold with human orthologue HsPI(4)K, demonstrates in vitro anti-Cryptosporidium activity (Cp CPE, EC50=52 nM).

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Biological Activity

EDI048 (EDI-048) is a specific, ATP-competitive, gastrointestinal-targeted Cryptosporidium PI(4)K (CpPI(4)K) inhibitor with IC50 of 4 nM, >300-fold with human orthologue HsPI(4)K, demonstrates in vitro anti-Cryptosporidium activity (Cp CPE, EC50=52 nM).
EDI048 is a potent CpPI(4)K inhibitor (IC50 = 5.2 nM) with anti-parasitic activity against both C. parvum and C. hominis, is active on Cryptosporidium in the gastrointestinal epithelium in the mouse model.
EDI048 demonstrated dose-dependent efficacy with a 0.3, 1.1 and 3.1 log reduction in oocyst shedding at 1, 3 and 10 mg kg−1 doses, respectively.
EDI048 is a soft drug in all tested preclinical species and had no human-specific metabolites, warranting further safety and efficacy profiling.
EDI048 blocks membrane biogenesis, preventing the formation of functional merozoites.

Physicochemical Properties

M.Wt 476.92
Formula C25H21ClN4O4
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

methyl 2-chloro-5-(N-methyl-3-(4-(methylcarbamoyl)phenyl)pyrazolo[1,5-a]pyridine-5-carboxamido)benzoate

References

1. Manjunatha UH, et al. Nat Microbiol. 2024 Oct 8. doi: 10.1038/s41564-024-01810-x.

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