Biological Activity
S1P3 receptor antagonist (Ki = 110 nM); inhibits S1P-induced Ca2+ release in HUVEC cells. Suppresses FTY-720-induced S1P3 receptor-mediated bradycardia in vivo. Also inhibits S1P-induced breast cancer stem cell expansion in vitro. Orally bioavailable.
Compound Libraries
TY 52156 is also offered as part of the Tocriscreen Plus. Find out more about compound libraries available from Tocris.
Technical Data
| M. Wt | 364.27 |
| Formula | C18H19Cl2N3O |
| Storage | Store at -20°C |
| Purity | ≥98% (HPLC) |
| CAS Number | 934369-14-9 |
| PubChem ID | 16046248 |
| InChI Key | XONRRGIRSGNWFP-UHFFFAOYSA-N |
| Smiles | ClC1=CC=C(/N=C(NNC2=CC=C(Cl)C=C2)/C(C(C)(C)C)=O)C=C1 |
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
All Tocris products are intended for laboratory research use only.
Solubility Data
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| DMSO | 36.43 | 100 | |
| ethanol | 36.43 | 100 |
Preparing Stock Solutions
The following data is based on the product molecular weight 364.27. Batch specific molecular weights may vary from batch to batch due to solvent of hydration, which will affect the solvent volumes required to prepare stock solutions.
| Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 1 mM | 2.75 mL | 13.73 mL | 27.45 mL |
| 5 mM | 0.55 mL | 2.75 mL | 5.49 mL |
| 10 mM | 0.27 mL | 1.37 mL | 2.75 mL |
| 50 mM | 0.05 mL | 0.27 mL | 0.55 mL |
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Product Datasheets
References
References are publications that support the products' biological activity.
Murakami et al (2010) Sphingosine 1-phosphate (S1P) regulates vascular contraction via S1P3 receptor: investigation based on a new S1P3 receptor antagonist. Mol.Pharmacol. 77 704 PMID: 20097776
Hirata et al (2014) Sphingosine-1-phosphate promotes expansion of cancer stem cells via S1PR3 by a ligand-independent Notch activation. Nat.Commun. 25 4806 PMID: 25254944
Keywords: TY 52156, supplier, TY52156, S1P3, receptors, antagonists, antagonism, sphingosine-1-phosphate, Sphingosine-1-phosphate, Receptors, Cancer, Stem, Cells, Sphingosine-1-phosphate, Receptors, Tocris Bioscience
