The S1P1 agonist SAR247799 is a biased agonist of the S1P1 sphingosine receptor, preferentially activating G protein signaling over the β-arrestin and internalization pathways.
|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.
 Maria Francesca Evaristi, et al. PLoS One. A G-protein-biased S1P1 agonist, SAR247799, improved LVH and diastolic function in a rat model of metabolic syndrome
 Luc Bergougnan, et al. Br J Clin Pharmacol. Endothelial-protective effects of a G-protein-biased sphingosine-1 phosphate receptor-1 agonist, SAR247799, in type-2 diabetes rats and a randomized placebo-controlled patient trial
 Patrick Grailhe, et al. FEBS Open Bio. A label-free impedance assay in endothelial cells differentiates the activation and desensitization properties of clinical S1P1 agonists
 Luc Bergougnan, et al. Br J Clin Pharmacol. First-in-human study of the safety, tolerability, pharmacokinetics and pharmacodynamics of single and multiple oral doses of SAR247799, a selective G-protein-biased sphingosine-1 phosphate receptor-1 agonist for endothelial protection
 Bruno Poirier, et al. Sci Signal. A G protein-biased S1P1 agonist, SAR247799, protects endothelial cells without affecting lymphocyte numbers
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