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DSM1465

Chemical Structure : DSM1465

CAS No.:

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DSM1465 (DSM-1465, DSM 1465)

Catalog No.: PC-23717Not For Human Use, Lab Use Only.

DSM1465 is a potent, selective inhibitor of P. falciparum dihydroorotate dehydrogenase (PfDHODH) with IC50 of 15 nM, inhibits P. falciparum 3D7 (Pf3D7) parasites in whole-cell assays with EC50 of 1.4 nM.

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Purity & Documentation Purity: >98% (HPLC)

Biological Activity

DSM1465 is a potent, selective inhibitor of P. falciparum dihydroorotate dehydrogenase (PfDHODH) with IC50 of 15 nM, inhibits P. falciparum 3D7 (Pf3D7) parasites in whole-cell assays with EC50 of 1.4 nM.
DSM1465 displays no inhibition of human DHODH (IC50>30 uM).
DSM1465 (1, 3, 10, and 30 mg/kg) showed impressive preliminary in vivo activity in the humanized SCID mouse P. falciparum efficacy model.

Physicochemical Properties

M.Wt 467.76
Formula C17H12ClF6N5O2
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

(R)-3-(1-(5-Chloro-6-(trifluoromethyl)pyridin-3-yl)-2,2,2-trifluoro-1-hydroxyethyl)-6-cyclopropyl-2-methyl-2,6-dihydro-7H-pyrazolo[4,3-d]pyrimidin-7-one

References

1. Zhe Nie, et al. J Med Chem. 2024 Dec 22. doi: 10.1021/acs.jmedchem.4c02394.

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