Razuprotafib (AKB-9778) is an effective selective inhibitor of ve-PTP (HPTPß) catalytic activity (IC50=17 pM), which promotes TIE2 activation, enhances ANG1-induced TIE2 activation, and stimulates phosphorylation of signal molecules in TIE2 pathway. Including AKT, eNOS, and ERK. Razuprotafib inhibited structure-related phosphatase PTP1B with an IC50 of 780 nM. Besides HPTPη (IC50=36 pM) and HPTPγ (100 pM), Razuprotafib showed good selectivity to VE-PTP.
|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 ≥ 60 mg/mL|
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