1315311-14-8
Chemical Structure
SAR247799
Synonym(s): S1P1 agonist 3
- CAS No.: 1315311-14-8
- Formula:C21H16ClN3O5
- Molecular Weight:425.82
IUPAC Name: 2-(4-(5-(3-chlorophenoxy)oxazolo[5,4-d]pyrimidin-2-yl)-2,6-dimethylphenoxy)acetic acid
InChIKey: WRBZNIUFAKIIQG-UHFFFAOYSA-N
SMILES: O=C(O)COC1=C(C)C=C(C2=NC3=CN=C(OC4=CC=CC(Cl)=C4)N=C3O2)C=C1C
Biological Activity: SAR247799 (S1P1 agonist 3) is an oral activity, selective G-protein-biased sphingosine-1 phosphate receptor-1 (S1P1 ) agonist, with EC50s rang from 12.6 to 493 nM in S1P1-overexpressing cells and HUVECs. SAR247799 can be used for the research of endothelial protection, including type-2 diabetes, metabolic syndrome[1][2][3][4].
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SAR247799 | 99.38% | SAR247799 (S1P1 agonist 3) is an oral activity, selective G-protein-biased sphingosine-1 phosphate receptor-1 (S1P1 ) agonist, with EC50s rang from 12.6 to 493 nM in S1P1-overexpressing cells and HUVECs. SAR247799 can be used for the research of endothelial protection, including type-2 diabetes, metabolic syndrome. | ||||||||||||||||||||
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References
- [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. [Content Brief]
- [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. [Content Brief]
- [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. [Content Brief]
- [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 [Content Brief]
