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Cat. No. M21193
SAR247799 Structure

S1P1 agonist 3

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Biological Activity

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.

Chemical Information
Molecular Weight 425.82
Formula C21H16ClN3O5
CAS Number 1315311-14-8
Form Solid
Solubility (25°C) DMSO 33.33 mg/mL
Storage -20°C
Conversion of different model animals based on BSA (PMID: 27057123)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
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.


[1] 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

[2] 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

[3] 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

[4] 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

[5] Bruno Poirier, et al. Sci Signal. A G protein-biased S1P1 agonist, SAR247799, protects endothelial cells without affecting lymphocyte numbers

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Keywords: SAR247799, S1P1 agonist 3 supplier, S1P Receptor, inhibitors, activators

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