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SAR247799

Name: SAR247799
Brand: TargetMol
SKU: T38716
Rating: 4.5 (1 reviews)

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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

😃Good

Catalog No. T38716Alias SAR 247799, S1P1 agonist 3Cas No. 1315311-14-8

Pack Size	Price	USA Warehouse	Global Warehouse	Quantity
5 mg	$1,199	7-10 days	7-10 days

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In Stock Estimated shipping dateUSA Warehouse[1-2 days] Global Warehouse[5-7 days]

All TargetMol products are for research purposes only and cannot be used for human consumption. We do not provide products or services to individuals. Please comply with the intended use and do not use TargetMol products for any other purpose.

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Product Introduction

Bioactivity

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].
Synonyms	SAR 247799, S1P1 agonist 3

Chemical Properties

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 mg/mL (46.97 mM), Sonication is recommended.

In Vivo Formulation

10% DMSO+40% PEG300+5% Tween-80+45% Saline: 2 mg/mL (4.7 mM), Sonication is recommeded.

Please add the solvents sequentially, clarifying the solution as much as possible before adding the next one. Dissolve by heating and/or sonication if necessary. Working solution is recommended to be prepared and used immediately. The formulation provided above is for reference purposes only. In vivo formulations may vary and should be modified based on specific experimental conditions.

Solution Preparation Table

DMSO

	1mg	5mg	10mg	50mg
1 mM	2.3484 mL	11.7421 mL	23.4841 mL	117.4205 mL
5 mM	0.4697 mL	2.3484 mL	4.6968 mL	23.4841 mL
10 mM	0.2348 mL	1.1742 mL	2.3484 mL	11.7421 mL
20 mM	0.1174 mL	0.5871 mL	1.1742 mL	5.8710 mL

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In Vivo Formulation Calculator (Clear solution)

Please enter your animal experiment information in the following box and click Calculate to obtain the mother liquor preparation method and in vivo formula preparation method:

For example, your dosage is 10 mg/kg Each animal weighs 20 g, and the dosage volume is 100 μL . TargetMol | Animal experiments

A total of 10 animals were administered, and the formula you used is 5% TargetMol | reagent

DMSO+30% PEG300+5% Tween 80+60% Saline/PBS/ddH₂O. So your working solution concentration is 2 mg/mL。

Mother liquor preparation method: 2 mg of drug dissolved in 50 μL DMSO TargetMol | reagent

(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 TargetMol | reagent

main solution, add 300 μLPEG300 TargetMol | reagent

mix well and clarify, then add 50 more μL Tween 80, mix well and clarify, then add 600 more μLSaline/PBS/ddH₂O TargetMol | reagent

mix well and clarify

For Reference Only. Please develop an appropriate dissolution method based on your laboratory animals and route of administration.

All types of co-solvents required for the protocol, such asDMSO, PEG300/ PEG400, Tween 80, SBE-β-CD, corn oil are available for purchase on the TargetMol website with a simple click.

Dose Conversion

You can also refer to dose conversion for different animals. More Dose Conversion

Tech Support

Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc