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

SAR247799 (Synonyms: S1P1 agonist 3)

Cat. No.: HY-115831
Handling Instructions

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

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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].

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

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.

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.
Molecular Weight

425.82

Formula

C21H16ClN3O5

CAS No.
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

Please store the product under the recommended conditions in the Certificate of Analysis.

Purity & Documentation
References
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SAR247799
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