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SAR247799
🥰Excellent
Catalog No. T38716Cas No. 1315311-14-8
Alias SAR 247799, S1P1 agonist 3
SAR247799 (S1P1 agonist 3) is a selective and G-protein-biased S1P1 agonist that activates downstream G-protein signaling pathways more preferentially than β-blocker proteins and internalized signaling pathways, activates S1P 1 on endothelial cells without causing receptor desensitization, and protects the endothelium without affecting lymphocyte populations, and can be used to study type 2 diabetes, endothelial dysfunction and vascular hyperpermeability.
SAR247799
🥰Excellent
Catalog No. T38716Alias SAR 247799, S1P1 agonist 3Cas No. 1315311-14-8
SAR247799 (S1P1 agonist 3) is a selective and G-protein-biased S1P1 agonist that activates downstream G-protein signaling pathways more preferentially than β-blocker proteins and internalized signaling pathways, activates S1P 1 on endothelial cells without causing receptor desensitization, and protects the endothelium without affecting lymphocyte populations, and can be used to study type 2 diabetes, endothelial dysfunction and vascular hyperpermeability.
| Pack Size | Price | Availability | Quantity |
|---|---|---|---|
| 5 mg | $1,462 | In Stock |
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Product Introduction
Bioactivity
Chemical Properties
| Description | SAR247799 (S1P1 agonist 3) is a selective and G-protein-biased S1P1 agonist that activates downstream G-protein signaling pathways more preferentially than β-blocker proteins and internalized signaling pathways, activates S1P 1 on endothelial cells without causing receptor desensitization, and protects the endothelium without affecting lymphocyte populations, and can be used to study type 2 diabetes, endothelial dysfunction and vascular hyperpermeability. |
| Targets&IC50 | Gi-mediated cAMP (S1P1, HEK293 cells):1.4 nM (EC50), β-arrestin recruitment (S1P1, HEK293 cells):15 nM (EC50) |
| In vitro | SAR247799 is a potent G protein–biased agonist of human S1P1 receptors in HEK293 cells. It showed an EC₅₀ of 1.4 nM in Gi-mediated cAMP inhibition assays, but a much weaker EC₅₀ of 15 nM for β-arrestin recruitment, indicating strong bias toward G protein signaling. In endothelial cells, SAR247799 (1–100 nM) upregulated eNOS and KLF2, promoting vascular protection[1]. |
| In vivo | In Zucker fa/fa rats (a type 2 diabetes model), oral administration of SAR247799 (0.002–0.24 mg/kg daily for 5 weeks) significantly improved arterial compliance, reduced urinary albumin excretion, and increased renal blood flow at low doses (0.007 mg/kg) without causing peripheral lymphopenia. The treatment also increased expression of endothelial genes (eNOS, KLF2), supporting its vascular-protective action via G protein–biased S1P1 activation[1]. |
| Alias | SAR 247799, S1P1 agonist 3 |
| Molecular Weight | 425.82 |
| Formula | C21H16ClN3O5 |
| Cas No. | 1315311-14-8 |
| Smiles | O=C(O)COC=1C(=CC(=CC1C)C2=NC3=CN=C(N=C3O2)OC=4C=CC=C(Cl)C4)C |
| Relative Density. | 1.412 g/cm3 (Predicted) |
Storage & Solubility Information
| Storage | keep away from moisture,keep away from direct sunlight | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature. | |||||||||||||||||||||||||
| Solubility Information | DMSO: 20.00 mg/mL (46.97 mM), Sonication is recommended. | |||||||||||||||||||||||||
Solution Preparation Table | ||||||||||||||||||||||||||
DMSO
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(mother liquor concentration of 40 mg/mL), if you need to configure a concentration that exceeds the solubility of the product, please contact us first.Preparation method for in vivo formula: Take 50 μL DMSO main solution, add 300 μLPEG300 mix well and clarify, then add 50 more μL Tween 80, mix well and clarify, then add 600 more μLSaline/PBS/ddH2O mix well and clarify
main solution, add 300 μLPEG300 mix well and clarify, then add 50 more μL Tween 80, mix well and clarify, then add 600 more μLSaline/PBS/ddH2O mix well and clarifyFor Reference Only. Please develop an appropriate dissolution method based on your laboratory animals and route of administration.
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