5.33062

S1P3 Receptor Antagonist, TY-52156

• Sinonimo/i: S1P3 Receptor Antagonist, TY-52156, S1P3 Antagonist, TY-52156, Sphingosine 1-phosphate Receptor Antagonist, TY-52156, TY52156, TY 52156, [1-Chloro-1-(4-chlorophenylhydrazono)]-3,3-dimethyl-2-butanone
• Formula empirica (notazione di Hill): C₁₈H₁₉Cl₂N₃O
• Numero CAS: 934369-14-9
• Peso molecolare: 364.27
• Codice UNSPSC: 12352200

Proprietà

• Saggio: ≥98% (HPLC)
• Livello qualitativo: 100
• Forma fisica: solid
• Produttore/marchio commerciale: Calbiochem^®
• Condizioni di stoccaggio: OK to freeze; protect from light
• Colore: orange
• Solubilità: DMSO: 50 mg/mL
• Temperatura di conservazione: −20°C

Descrizione

Descrizione generale

A cell-permeable hydrazonamide derivative that acts as a selective and competitive antagonist of S1P3 receptor (K_i = 110 nM) and suppresses S1P-induced expansion of A549, LNCaP, U251MG, and OVCAR-5 cancer cells (~ 10 µM). Displays about 30-fold lower effect on S1P1, S1P2, S1P4, or S1P5 receptors and does not affect 24 different G-protein coupled receptors (~10 µM). Shown to block S1P-induced expression of Hes1 and reduce ALDH-positive cell population. Inhibits the tumorigenicity of SphK1-overexpressing ALDH-positive cells following chronic administration over a period of 6 weeks. Preferentially inhibits S1P-induced increase in [Ca2+]i and Rho activation in vascular smooth muscle cells. Shown to reduce S1P3 receptor-induced bradycardia in vivo in rats and diminishes coronary flow in perfused rat heart. Also shown to relax cerebral arteries precontracted with S1P.

Please note that the molecular weight for this compound is batch-specific due to variable water content. Please refer to the vial label or the certificate of analysis for the batch-specific molecular weight. The molecular weight provided represents the baseline molecular weight without water.

A hydrazonamide derivative that suppresses the S1P-induced cancer stem cell expansion effects in multiple human cancer cell lines including, breast cancer MCF-7 cells, lung cancer A549 cells, glioma U251MG cells and ovarian cancer OVCAR-5 cells at 10 µM. Significantly inhibits the tumorigenicity of SphK1-overexpressing ALDH-positive cells after chronic continuous injection for 6 weeks (167mg/ml) in a mouse xenograft model. In addition, shown to suppress the S1P-induced effects such as Ca2+ increase and Rho activation in vascular smooth muscle cells and decrease of coronary flow in isolated perfused rat hearts.

Azioni biochim/fisiol

Primary Target
S1P3

Confezionamento

Packaged under inert gas

Attenzione

Toxicity: Standard Handling (A)

Ricostituzione

Following reconstitution, aliquot and freeze (-70°C). Stock solutions are stable for up to 4 weeks at -70°C.

Altre note

Hirata, N., et al. 2014, Nat. Comm.5, in press.
Murakami, A., et al. 2010. Mol. Pharm.77, 704.

Note legali

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany

Informazioni sulla sicurezza

• Codice della classe di stoccaggio: 11 - Combustible Solids
• Classe di pericolosità dell'acqua (WGK): WGK 3
• Punto d’infiammabilità (°F): Not applicable
• Punto d’infiammabilità (°C): Not applicable