2. GPCR/G Protein
  3. LPL Receptor
  4. SAR247799

SAR247799  (Synonyms: S1P1 agonist 3)

Cat. No.: HY-115831 Purity: 97.21%
SDS COA Handling Instructions Technical Support

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.

For research use only. We do not sell to patients.

SAR247799 Chemical Structure

SAR247799 Chemical Structure

CAS No. : 1315311-14-8

Size Price Stock Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
 In-stock
Solution
10 mM * 1 mL in DMSO In-stock
Solid
5 mg In-stock
10 mg In-stock
25 mg In-stock
50 mg In-stock
100 mg In-stock
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Customer Review

Based on 1 publication(s) in Google Scholar

SAR247799 Related Antibodies

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  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

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].

IC50 & Target[1]

S1PR1

12.6-493 nM (EC50)

In Vitro

SAR247799 (0, 0.003, 0.01, 0.03, 0.1, 0.3, 1, 3, 10 μM; 10 min) induces a concentration-dependent phosphorylation of extracellular-regulated kinase-1/2 (Erk1/2) and protein kinase B (Akt) in HUVECs[1].
SAR247799 (0-10 μM, 8 min) induces impedance change in HUVECs in a dose-dependent manner[1].
SAR247799 (1 μM, 1st) does not cause desensitization demonstrated by Ca2+ flux assay in S1P1-Chinese hamster ovary (CHO) cells[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

SAR247799 Related Antibodies
In Vivo

SAR247799 (1 and 3 mg/kg; p.o.; 1 h before renal occlusion) dose dependently reduces the severity of ischemia/reperfusion (I/R)–induced acute kidney injury[1].
SAR247799 (0.3, 1, 3 mg/kg; i.v.) dose dependently increases the coronary conductance ratio in pig model of coronary endothelial dysfunction[1].
SAR247799 (30-min intravenous administration; 8- to 10-week-old farm pig) exposure (Cmax and AUC) increases with dose in pigs. Pharmacokinetic parameters [1]:

Dose (mg/kg) N Cmax (g/mL) Tmax (h) Tlast (h) AUC0-last (g.h/mL) Cl (L/h/kg) Vss (L/kg) T1/2z (h)
1 4 2.08 (8) 0.5 [0.5] [8-48] 11.8 (46) 0.113 (75) 0.516 (11) 5.62 (57)
3 7 8.10 (12) 0.5 [0.5] [24-72] 42.2 (23) 0.0754 (30) 0.446 (16) 6.21 (28)
10 3 36.7 (5) 0.5 [0.5-0.75] 72 294 (13) 0.0343 (13) 0.338 (7) 7.73 (8)
30 6 112 (27) 0.5 [0.5- 1.0] [48-72] 908 (16) 0.0338 (18) 0.294 (11) 7.35 (11)
Mean values with (CV%) except Tmax, which is expressed as median value with [range] and Tlast as [range]. Cmax, maximum concentration. Tmax, time at which maximum concentration achieved. Tlast, last time point sampled. AUC0-last, area under curve from 0 to last time point. Cl, clearance. Vss, volume at steady state or volume of distribution. T1/2z, elimination half-life. N, number of animals.

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Acute kidney injury rats (12 to 15-week-old Fischer rats)[1]
Dosage: 1 and 3 mg/kg
Administration: P.o.; administered 1 hour before renal occlusion.
Result: Inhibited the increase in serum creatinine (89 and 96% at 1 and 3 mg/kg) and urea (61 and 85% at 1 and 3 mg/kg).
Protected renal proximal tubules against necrosis and blunted the development of interstitial hemorrhage.
Animal Model: Acute kidney injury rats (8- to 12-week-old Fischer rats)[1]
Dosage: 3 mg/kg
Administration: P.o.; twice a day for 7 days and twice a day for 7 day
Result: Showed a dosedependent trend for reducing macrophage.
Clinical Trial
Molecular Weight

425.82

Formula

C21H16ClN3O5
CAS No.
Appearance

Solid

Color

Off-white to light yellow

SMILES

O=C(O)COC1=C(C)C=C(C2=NC3=CN=C(OC4=CC=CC(Cl)=C4)N=C3O2)C=C1C
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

4°C, sealed storage, away from moisture and light

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)

Solvent & Solubility
In Vitro: 

DMSO : 33.33 mg/mL (78.27 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.3484 mL 11.7421 mL 23.4841 mL
5 mM 0.4697 mL 2.3484 mL 4.6968 mL
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

  • Molarity Calculator

  • Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass
=
Concentration
×
Volume
×
Molecular Weight *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

  • Protocol 1

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% Saline

    Solubility: ≥ 2.5 mg/mL (5.87 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

    Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
  • Protocol 2

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in Saline)

    Solubility: ≥ 2.5 mg/mL (5.87 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

    Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO +
% 
+
%
Tween-80 +
%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Purity & Documentation
References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.3484 mL 11.7421 mL 23.4841 mL 58.7103 mL
5 mM 0.4697 mL 2.3484 mL 4.6968 mL 11.7421 mL
10 mM 0.2348 mL 1.1742 mL 2.3484 mL 5.8710 mL
15 mM 0.1566 mL 0.7828 mL 1.5656 mL 3.9140 mL
20 mM 0.1174 mL 0.5871 mL 1.1742 mL 2.9355 mL
25 mM 0.0939 mL 0.4697 mL 0.9394 mL 2.3484 mL
30 mM 0.0783 mL 0.3914 mL 0.7828 mL 1.9570 mL
40 mM 0.0587 mL 0.2936 mL 0.5871 mL 1.4678 mL
50 mM 0.0470 mL 0.2348 mL 0.4697 mL 1.1742 mL
60 mM 0.0391 mL 0.1957 mL 0.3914 mL 0.9785 mL
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SAR247799 Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

SAR2477991315311-14-8S1P1 agonist 3SAR 247799SAR-247799LPL ReceptorLysophospholipid Receptortype-2 diabetesmetabolic syndromeendothelial protectionHUVECspigratInhibitorinhibitorinhibit

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