Lanifibranor (IVA-337) is a peroxisome proliferator-activated receptors (PPAR) agonist, with EC50s of 1.5, 0.87 and 0.21 μM for human PPARα, PPARσ and PPARγ, respectively. Lanifibranor (100 mg/kg) administration results in reduced body weight compare with vehicle controls (p<0.05).
|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 ≥ 70 mg/mL|
 Benaissa Boubia, et al. J Med Chem. Design, Synthesis, and Evaluation of a Novel Series of Indole Sulfonamide Peroxisome Proliferator Activated Receptor (PPAR) α/γ/δ Triple Activators: Discovery of Lanifibranor, a New Antifibrotic Clinical Candidate
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Inolitazone dihydrochloride (Efatutazone dihydrochloride) is a PPARγ agonist with high affinity, activity dependent on PPARγ, inhibiting growth, IC50 is 0.8 nM.
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