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TY 52156
- Soluble in DMSO
- MF: C18H19Cl2N3O
- MW: 364.27
Description
TY 52156 is a selective, competitive S1P3 receptor antagonist with oral activity in preclinical models. It blocks S1P3-mediated vascular and cardiac responses, including Rho-dependent calcium signaling and S1P-associated reductions in coronary blood flow.
Sphingosine-1-phosphate receptors regulate vascular tone, endothelial signaling, immune trafficking and cardiac rhythm. TY 52156 is a useful tool for separating S1P3-mediated cardiovascular effects from other S1P receptor subtypes in receptor and in vivo pharmacology assays.
Key Features
- Selective S1P3 receptor antagonist
- Competitive antagonist of S1P3-mediated signaling
- Inhibits Rho-dependent activation and calcium responses
- Blocks FTY720-induced S1P3-mediated bradycardia in vivo
Applications
- S1P receptor subtype pharmacology
- Cardiovascular signaling and coronary flow studies
- Calcium and Rho pathway assays
- Evaluation of S1P3 contributions to FTY720-related effects
More Information
| Parent CAS No. | 934369-14-9 |
|---|---|
| Chemical Name | N,N'-bis(4-chlorophenyl)-3,3-dimethyl-2-oxobutanehydrazonamide |
| SMILES | C(/NC1=CC=C(Cl)C=C1)(=NNC1=CC=C(Cl)C=C1)C(=O)C(C)(C)C |
| MFCD | N.A. |
| InChi | InChI=1S/C18H19Cl2N3O/c1-18(2,3)16(24)17(21-14-8-4-12(19)5-9-14)23-22-15-10-6-13(20)7-11-15/h4-11,22H,1-3H3,(H,21,23) |
| InChiKey | XONRRGIRSGNWFP-UHFFFAOYSA-N |
| CID | 16046248 |
| Short Description | S1P3 antagonist |
References
- A. Murakami et al. Sphingosine 1-phosphate (S1P) regulates vascular contraction via S1P3 receptor: investigation based on a new S1P3 receptor antagonist. Mol Pharmacol. 2010 Apr;77(4):704-13.
- N.J. Pyne et al. Selectivity and specificity of sphingosine 1-phosphate receptor ligands: "off-targets" or complex pharmacology? Front Pharmacol. 2011 May 31;2:26.
- K. Sobel et al. Sphingosine 1-phosphate (S1P) receptor agonists mediate pro-fibrotic responses in normal human lung fibroblasts via S1P2 and S1P3 receptors and Smad-independent signaling. J Biol Chem. 2013 May 24;288(21):14839-51.
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