Shopping Cart
- Remove All
- Your shopping cart is currently empty
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 |
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 | β-arrestin recruitment (S1P1, HEK293 cells):15 nM (EC50), Gi-mediated cAMP (S1P1, HEK293 cells):1.4 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 | 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
|
Copyright © 2015-2025 TargetMol Chemicals Inc. All Rights Reserved.