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ML471

Chemical Structure : ML471

CAS No.: 2226227-77-4

ML471 (ML-471)

Catalog No.: PC-23599Not For Human Use, Lab Use Only.

ML471 is a potent, selective reaction hijacking inhibitor of P.falciparum tyrosine tRNA synthetase (PfTyrRS, PfYRS), inhibits growth of asexual blood stage P. falciparum (3D7 strain) in a 72-h exposure assay with IC50 of 2.8 nM.

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Purity & Documentation Purity: >98% (HPLC)

Biological Activity

ML471 is a potent, selective reaction hijacking inhibitor of P.falciparum tyrosine tRNA synthetase (PfTyrRS, PfYRS), inhibits growth of asexual blood stage P. falciparum (3D7 strain) in a 72-h exposure assay with IC50 of 2.8 nM.
ML471 has no inhibitory activity against human ubiquitin-activating enzyme (UAE) in vitro.
ML471 exhibits low nanomolar activity against asexual blood stage P. falciparum and potent activity against liver stage parasites, gametocytes and transmissible gametes.
ML471 is well-tolerated and shows single dose oral efficacy in the SCID mouse model of P. falciparum malaria.

Physicochemical Properties

M.Wt 388.40
Formula C13H20N6O6S
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

((2R,3S,4R,5R)-5-(4-amino-3-isopropyl-1H-pyrazolo[3,4-d]pyrimidin-1-yl)-3,4-dihydroxytetrahydrofuran-2-yl)methyl sulfamate

References

1. Xie SC, et al. PLoS Pathog. 2024 Dec 9;20(12):e1012429.

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