NOD-IN-1 (compound 4) is potent mixed inhibitor of NOD1 and NOD2, displaying a balanced inhibitory activity on both targets in the low micromolar range. NOD-IN-1 (IC50 (NOD1)=5.74 μM; IC50 (NOD2)=6.45 μM) is identified as the best of the series, possessing NOD1- and NOD2-inhibitory activities in the lower micromolar range. These results show that NOD-IN-1 is 7-fold less potent than Noditinib-1 in terms of NOD1 inhibition and completely devoid of selective activity for NOD1 or NOD2 as opposed to Noditinib-1. NOD-IN-1 exhibits balanced dual activities of less than 10 μM on the two targets.
|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.
|Solubility||DMSO ≥ 50 mg/mL|
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