5.33062
S1P3 Receptor Antagonist, TY-52156
别名:
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
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关于此项目
经验公式（希尔记法）:
C18H19Cl2N3O
化学文摘社编号:
分子量:
364.27
MDL number:
UNSPSC Code:
41116158
NACRES:
NA.77
InChI key
XONRRGIRSGNWFP-UHFFFAOYSA-N
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)
SMILES string
Clc1ccc(cc1)N\N=C(\Nc2ccc(cc2)Cl)/C(=O)C(C)(C)C
assay
≥98% (HPLC)
form
solid
manufacturer/tradename
Calbiochem®
storage condition
OK to freeze, protect from light
color
orange
solubility
DMSO: 50 mg/mL
storage temp.
−20°C
Quality Level
General description
A cell-permeable hydrazonamide derivative that acts as a selective and competitive antagonist of S1P3 receptor (Ki = 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.
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.
Biochem/physiol Actions
Primary Target
S1P3
S1P3
Packaging
Packaged under inert gas
Preparation Note
Following reconstitution, aliquot and freeze (-70°C). Stock solutions are stable for up to 4 weeks at -70°C.
Other Notes
Hirata, N., et al. 2014, Nat. Comm.5, in press.
Murakami, A., et al. 2010. Mol. Pharm.77, 704.
Murakami, A., et al. 2010. Mol. Pharm.77, 704.
Legal Information
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
Disclaimer
Toxicity: Standard Handling (A)
存储类别
11 - Combustible Solids
wgk
WGK 3
flash_point_f
Not applicable
flash_point_c
Not applicable
法规信息
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