Stiripentol is an LDH inhibitor. Stiripentol (300 mg/kg ip) had a small effect on high-voltage spikes in the kainate model. Stiripentol (500 mM) inhibited the lactate-to-pyruvate conversion as well as the pyruvate-to-lactate conversion by both human LDHs. Lineweaver-Burk plots revealed that the inhibition by stiripentol was noncompetitive, suggesting that stiripentol binds to the LDHs at a different site with lactate and pyruvate.
|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 ≥ 30 mg/mL|
|Related Cytochrome P450 (e.g. CYP17) Products|
Bergaptol is a hydroxylated psoralen that acts as a potent inhibitors of debenzylation activity of CYP3A4 enzyme with an IC50 value of 24.92 uM.
ε-Viniferin is a potent inhibitor for all the CYP family, with Ki values from 0.5-20 μM.
Rhapontigenin is a selective inactivator of cytochrome P450 1A1 with IC50 of 400 nM.
(Rac)-Brassinazole is a brassinosteroid (BR) biosynthesis inhibitor.
Apigenin is a protein kinase inhibitor.
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