SEW2871A potent selective EDG-1 inhibitor

SEW2871 (CAS 256414-75-2)

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Application: A potent selective EDG-1 inhibitor
CAS Number: 256414-75-2
Purity: >98%
Molecular Weight: 440.36
Molecular Formula: C20H10F6N2OS
Supplemental Information: This is classified as a Dangerous Good for transport and may be subject to additional shipping charges.
* Refer to Certificate of Analysis for lot specific data (including water content).
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SEW2871 is a small molecule selective agonist of EDG-1 (Sphingosine-1-phosphate receptor 1; S1P1), a protein involved in signaling and regulation of heart rate, coronary artery caliber, and lymphocyte recirculation. SEW2871 has been used as a tool for investigating the role of the EDG-1 receptor in cardiovascular regulation, and specifically for its role in ischemia/reperfusion injury. An antiinflammatory behavior is produced by SEW2871 activation of the EDG-1 receptor, showing an inhibition of monocyte adhesion to endothelial cells upon this activation.


References

1. Kluk, M.J. and Hla, T. 2002. Biochim. Biophys. Acta. 1582: 72-80. PMID: 12069812
2. Sanna, M.G., et al. 2004. J. Biol. Chem. 279: 13839-13848. PMID: 14732717
3. Hale, J.J., et al. 2004. J. Med. Chem. 47: 6662-6665. PMID: 15615513
4. Bolick, D.T., et al. 2005. Arterioscler. Thromb. Vasc. Biol. 25: 976-981. PMID: 15761190
5. Whetzel, A.M., et al. 2006. Circ. Res. 99: 731-739. PMID: 16960101

Physical State :
Solid
Solubility :
Soluble in DMSO (≥10 mg/ml), ethanol (20 mM), and DMF (~30 mg/ml). Insoluble in water.
Storage :
Store at -20° C
Melting Point :
94.5-95.3° C
Boiling Point :
490.32° C at 760 mmHg (Predicted)
Density :
1.42 g/cm3 (Predicted)
Refractive Index :
n20D 1.54 (Predicted)
IC50 :
EDG-3: IC50 >10 nM (human); EDG-1: EC5050 = 13 nM (human); S1P1: EC5050 = 20.7 nM (murine); EDG-1: IC50 = 37 nM (human); EDG-8: IC50 = 4.6 µM (human)
For Research Use Only. Not Intended for Diagnostic or Therapeutic Use.
WGK Germany :
3
PubChem CID :
4077460
MDL Number :
MFCD00096600
SMILES :
C1=CC=C(C=C1)C2=C(SC(=C2)C3=NC(=NO3)C4=CC(=CC=C4)C(F)(F)F)C(F)(F)F

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Certificate of Analysis

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