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DDD489

Chemical Structure : DDD489

CAS No.: 3003871-42-6

DDD489 (DDD-489)

Catalog No.: PC-23267Not For Human Use, Lab Use Only.

DDD489 is a potent, selective Cryptosporidium lysyl-tRNA synthetase (CpKRS) inhibitor with IC50 of 0.85 uM, and C. parvum EC50 of 0.04 uM, shows anti-cryptosporidials activity.

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Purity & Documentation Purity: >98% (HPLC)

Biological Activity

DDD489 is a potent, selective Cryptosporidium lysyl-tRNA synthetase (CpKRS) inhibitor with IC50 of 0.85 uM, and C. parvum EC50 of 0.04 uM, shows anti-cryptosporidials activity.
DDD489 is selective over HsKRS (IC50=22 uM) and shows low cytotoxicity in HsHepG2 cells.
DDD489 is effective in key cryptosporidiosis mouse models.
DDD489 (15 mg/kg, BID) reduce parasite shedding and diarrheal scores in calves.
Overexpression or mutation of CpKRS (A309L mutation) confers resistance to DDD489.
DDD489 binds in a similar pose in the ATP site of CpKRS.

Physicochemical Properties

M.Wt 382.31
Formula C15H16F6N4O
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

2-amino-4-(trifluoromethyl)-6-(((1R,3S)-3-(trifluoromethyl)cyclohexyl)methyl)-6,7-dihydro-5H-pyrrolo[3,4-d]pyrimidin-5-one

References

1. Caldwell N, et al. Sci Transl Med. 2024 Oct 23;16(770):eadm8631.

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