NDI-091143 is a novel potent inhibitor of human ATP-citrate lyase with an IC50 of 2.1 nM (ADP-Glo assay). NDI-091143 inhibits ACLY catalysis allosterically, by stabilizing large conformational changes in the citrate domain. The thermal shift data are consistent with limited proteolysis experiments using full-length ACLY, in which NDI-091143 together with Mg-ATP provided the greatest protection against digestion by chymotrypsin.
|Solubility (25°C)||DMSO ≥ 60 mg/mL|
Powder -20°C 3 years ; 4°C 2 years
In solvent -80°C 6 months ; -20°C 1 month
|Body Surface Area (m2)||0.007||0.025||0.15||0.05||0.02||0.5|
|Animal A (mg/kg) = Animal B (mg/kg) multiplied by||Animal B Km|
|Animal A Km|
For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.
 Carlotta Granchi. Trends Pharmacol Sci. Discovery of Allosteric Inhibition of Human ATP-Citrate Lyase
 Jia Wei, et al. Nature. An Allosteric Mechanism for Potent Inhibition of Human ATP-citrate Lyase
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