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Submit ReviewTY 52156 is an 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.
TY 52156 is also offered as part of the Tocriscreen 2.0 Max. Find out more about compound libraries available from Tocris.
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.
Tocris products are intended for laboratory research use only, unless stated otherwise.
Solvent | Max Conc. mg/mL | Max Conc. mM | |
---|---|---|---|
Solubility | |||
DMSO | 36.43 | 100 | |
ethanol | 36.43 | 100 |
The following data is based on the product molecular weight 364.27. Batch specific molecular weights may vary from batch to batch due to the degree 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 |
References are publications that support the biological activity of the product.
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
If you know of a relevant reference for TY 52156, please let us know.
Keywords: TY 52156, TY 52156 supplier, TY52156, S1P3, receptors, antagonists, antagonism, sphingosine-1-phosphate, Sphingosine-1-phosphate, Receptors, Cancer, Stem, Cells, 5328, Tocris Bioscience
Citations are publications that use Tocris products. Selected citations for TY 52156 include:
Rosalinda et al (2021) Intracellular Sphingosine-1-Phosphate Receptor 3 Contributes to Lung Tumor Cell Proliferation. Cell Physiol Biochem 55 539-552 PMID: 34473432
Rosalinda et al (2022) S1P-Induced TNF-α and IL-6 Release from PBMCs Exacerbates Lung Cancer-Associated Inflammation. Cells 11 PMID: 36010601
Ma et al (2017) A Brain-Region-Specific Neural Pathway Regulating Germinal Matrix Angiogenesis. Dev Cell 41 366 PMID: 28535372
Schuhmann et al (2015) Fingolimod (FTY720-P) Does Not Stabilize the Blood-Brain Barrier under Inflammatory Conditions in an in Vitro Model. J Neurosci 16 29454 PMID: 26690412
Hoffmann et al (2015) Fingolimod induces neuroprotective factors in human astrocytes. J Neuroinflammation 12 184 PMID: 26419927
Hübner et al (2018) Wnt/β-catenin signaling regulates VE-cadherin-mediated anastomosis of brain capillaries by counteracting S1pr1 signaling. Nat Commun 9 4860 PMID: 30451830
Heo and Im (2019) Pro-Inflammatory Role of S1P3 in Macrophages. Biomol Ther (Seoul) PMID: 30917625
Do you know of a great paper that uses TY 52156 from Tocris? Please let us know.
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