[CAS NO. 256414-75-2] SEW2871
PRODUCTS SPECIFICATIONS [256414-75-2]
DESCRIPTION [256414-75-2]
Overview
| MDL | MFCD00096600 |
|---|---|
| Molecular Weight | 440.36 |
| Molecular Formula | C20H10F6N2OS |
| SMILES | FC(C1=CC(C2=NOC(C3=CC(C4=CC=CC=C4)=C(C(F)(F)F)S3)=N2)=CC=C1)(F)F |
Summary
SEW2871 is an orally active, potent, highly selective S1P1 (sphingosine-1-phosphate type 1 receptor) agonist, with an EC 50 of 13.8 nM. SEW2871 activates ERK , Akt , and Rac signaling pathways and induces S1P1 internalization and recycling. SEW2871 reduces lymphocyte numbers in blood. SEW2871 can be used for the research of diabetes, Alzheimer’s disease, liver fibrosis, and inflammatory responses [1] [2] .
IC50 & Target
|
S1PR1 13.8 nM (EC 50 ) |
In Vitro
SEW2871 exerts a powerful migratory effect by increasing smooth muscle α-actin, procollagen αI and αIII, and total hydroxyproline contents in LX-2 cells (a human hepatic stellate cell line) [2] .
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
In Vivo
SEW2871 (20 mg/kg, Gavage, once daily for 2 weeks) ameliorates established experimental colitis in IL-10
–/–
mice
[3]
.
SEW2871 (0.5 mg/kg, IP, daily for 2 weeks) inhibited β amyloid (Aβ
1-42
)-induced spatial memory impairment and hippocampal neuronal loss in a rat model of Alzheimer’s disease
[2]
.
SEW2871 (0-0.3 mg/kg, IV) attenuates LPS-induced acute inflammatory lung injury, produces dose-dependent alveolar and vascular barrier protection in C57Bl/6 mice
[2]
.
SEW2871 is effective in protecting kidneys against ischaemia-reperfusion injury by reducing CD4
+
T cell infiltration in mice
[3]
.
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
| Animal Model: | IL-10 –/– (interleukin (IL)-10 gene-deficient) mice, a murine model of Crohn's disease (CD) [3] |
| Dosage: | 20 mg/kg |
| Administration: | Gavage, once daily for 2 weeks |
| Result: | Ameliorated established colitis in IL-10 –/– mice, associated with a reduction of serum amyloid A concentration, a decreased colon MPO concentration, a depletion of the peripheral CD4 + CD45 + T cells and a reduction of the homing of T cells into colon LP. Suppressed typical cytokines of T helper type 1 (Th1) and Th17 cells and p-STAT-3 expression, and significantly decreased TNF-α, IFN-γ, IL-1β and IL-17A mRNA levels. |
Appearance
Solid
Shipping
Room temperature in continental US; may vary elsewhere.
Storage
| Powder | -20°C | 3 years |
|---|---|---|
| In solvent | -80°C | 6 months |
| -20°C | 1 month |
Solvent & Solubility
DMSO : 25 mg/mL ( 56.77 mM ; Need ultrasonic)
Stock Solutions
| Concentration Solvent Mass | 1 mg | 5 mg | 10 mg |
|---|
| 1 mM | 2.2709 mL | 11.3543 mL | 22.7087 mL |
| 5 mM | 0.4542 mL | 2.2709 mL | 4.5417 mL |
| 10 mM | 0.2271 mL | 1.1354 mL | 2.2709 mL |
-
1.
-
2.
Add each solvent one by one: 10% DMSO >> 90% corn oil
Solubility: ≥ 2.08 mg/mL (4.72 mM); Clear solution
References
- [1] Park SJ, et al. Sphingosine 1-Phosphate Receptor Modulators and Drug Discovery. Biomol Ther (Seoul). 2017 Jan 1;25(1):80-90.
- [2] Jo E, et al. S1P1-selective in vivo-active agonists from high-throughput screening: off-the-shelf chemical probes of receptor interactions, signaling, and fate. Chem Biol. 2005 Jun;12(6):703-15.
- [3] Dong J, et al. Oral treatment with SEW2871, a sphingosine-1-phosphate type 1 receptor agonist, ameliorates experimental colitis in interleukin-10 gene deficient mice. Clin Exp Immunol. 2014 Jul;177(1):94-101.
