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SAR247799

Catalog No. T38716 CAS 1315311-14-8

Synonyms: SAR247799, S1P1 agonist 3

SAR247799 (S1P1 agonist 3) is an orally-active, selective G-protein-biased agonist for the sphingosine-1 phosphate receptor-1 (S1P1). It demonstrates EC50 values ranging from 12.6 to 493 nM in S1P1-overexpressing cells and HUVECs. SAR247799 holds promise as a valuable tool for investigating endothelial protection, particularly in the context of type-2 diabetes and metabolic syndrome[4].

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SAR247799, CAS 1315311-14-8

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Description	SAR247799 (S1P1 agonist 3) is an orally-active, selective G-protein-biased agonist for the sphingosine-1 phosphate receptor-1 (S1P1). It demonstrates EC50 values ranging from 12.6 to 493 nM in S1P1-overexpressing cells and HUVECs. SAR247799 holds promise as a valuable tool for investigating endothelial protection, particularly in the context of type-2 diabetes and metabolic syndrome[4].
Targets&IC50	S1PR1:12.6-493 nM (EC50)
In vitro	SAR247799, at varying concentrations (0, 0.003, 0.01, 0.03, 0.1, 0.3, 1, 3, 10 μM; for 10 minutes), triggers a dose-dependent phosphorylation of extracellular-regulated kinase-1/2 (Erk1/2) and protein kinase B (Akt) in HUVECs[1]. Furthermore, at concentrations ranging from 0 to 10 μM over 8 minutes, it prompts a dose-dependent change in impedance in HUVECs[1]. At a concentration of 1 μM and first exposure, SAR247799 does not induce desensitization as illustrated by the Ca2+ flux assay in S1P1-Chinese hamster ovary (CHO) cells[1].
In vivo	SAR247799 was investigated in various models for its potential therapeutic effects. Administered orally one hour prior to inducing renal occlusion at doses of 1 and 3 mg/kg, it significantly mitigated the severity of ischemia/reperfusion (I/R)–induced acute kidney injury by dose-dependently decreasing serum creatinine and urea levels, protecting renal proximal tubules from necrosis, and reducing interstitial hemorrhage development. Furthermore, intravenous doses of SAR247799 (0.3, 1, 3 mg/kg) enhanced coronary conductance ratio in a pig model of coronary endothelial dysfunction, indicating improved coronary flow. Pharmacokinetic analysis revealed that the exposure of SAR247799, assessed by peak plasma concentration (Cmax) and area under the concentration-time curve (AUC), increased with dose across tested ranges, demonstrating dose-dependent pharmacokinetics in pigs. The study utilized acute kidney injury rat models and farm pigs to evaluate the compound's efficacy and pharmacokinetics, highlighting its potential in treating renal injuries and coronary endothelial dysfunction without providing detailed pharmacokinetic values for brevity and focus on its therapeutic applications.

Synonyms	SAR247799, S1P1 agonist 3
Molecular Weight	425.83
Formula	C21H16ClN3O5
CAS No.	1315311-14-8

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

References and Literature

1. Poirier B, et al. A G protein-biased S1P1 agonist, SAR247799, protects endothelial cells without affecting lymphocyte numbers. Sci Signal. 2020 Jun 2;13(634):eaax8050. 2. Evaristi MF, et al. A G-protein-biased S1P1 agonist, SAR247799, improved LVH and diastolic function in a rat model of metabolic syndrome. PLoS One. 2022 Jan 14;17(1):e0257929. 3. Bergougnan L, et al. 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. Br J Clin Pharmacol. 2021 May;87(5):2303-2320. 4. Bergougnan L, et al. 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. Br J Clin Pharmacol. 2021 Feb;87(2):598-611.

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Keywords

SAR247799 1315311-14-8 SAR 247799 S1P1 agonist 3 SAR-247799 inhibitor inhibit

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