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533062 S1P3 Receptor Antagonist, TY-52156 - Calbiochem

Overview

Replacement Information

Key Specifications Table

Empirical Formula
C₁₈H₁₉Cl₂N₃O

Products

Catalog NumberPackaging Qty/Pack
5.33062.0001 Glass bottle 10 mg
Description
OverviewA 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.
Catalogue Number533062
Brand Family Calbiochem®
SynonymsS1P3 Antagonist, TY-52156, Sphingosine 1-phosphate Receptor Antagonist, TY-52156, TY52156, TY 52156, [1-Chloro-1-(4-chlorophenylhydrazono)]-3,3-dimethyl-2-butanone
DescriptionS1P3 Receptor Antagonist, TY-52156
References
ReferencesHirata, N., et al. 2014, Nat. Comm. 5, in press.
Murakami, A., et al. 2010. Mol. Pharm. 77, 704.
Product Information
FormOrange solid
Hill FormulaC₁₈H₁₉Cl₂N₃O
Chemical formulaC₁₈H₁₉Cl₂N₃O
Quality LevelMQ100
Applications
Biological Information
Primary TargetS1P3
Purity≥98% by HPLC
Physicochemical Information
Dimensions
Materials Information
Toxicological Information
Safety Information according to GHS
Safety Information
Product Usage Statements
Storage and Shipping Information
Ship Code Shipped at Ambient Temperature or with Blue Ice or with Dry Ice
Toxicity Standard Handling
Storage -20°C
Protect from Light Protect from light
Do not freeze Ok to freeze
Special InstructionsFollowing reconstitution, aliquot and freeze (-70°C). Stock solutions are stable for up to 4 weeks at -70°C.
Packaging Information
Packaged under inert gas Packaged under inert gas
Transport Information
Supplemental Information
Specifications
Global Trade Item Number
Catalog Number GTIN
5.33062.0001 04055977282054

Documentation

S1P3 Receptor Antagonist, TY-52156 - Calbiochem SDS

Title

Safety Data Sheet (SDS) 

References

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

Note that this data sheet is not lot-specific and is representative of the current specifications for this product. Please consult the vial label and the certificate of analysis for information on specific lots. Also note that shipping conditions may differ from storage conditions.

Revision09-September-2016 JSW
SynonymsS1P3 Antagonist, TY-52156, Sphingosine 1-phosphate Receptor Antagonist, TY-52156, TY52156, TY 52156, [1-Chloro-1-(4-chlorophenylhydrazono)]-3,3-dimethyl-2-butanone
DescriptionA 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.
FormOrange solid
Intert gas (Yes/No) Packaged under inert gas
Chemical formulaC₁₈H₁₉Cl₂N₃O
Purity≥98% by HPLC
SolubilityDMSO (50 mg/ml)
Storage Protect from light
-20°C
Do Not Freeze Ok to freeze
Special InstructionsFollowing reconstitution, aliquot and freeze (-70°C). Stock solutions are stable for up to 4 weeks at -70°C.
Toxicity Standard Handling
ReferencesHirata, N., et al. 2014, Nat. Comm. 5, in press.
Murakami, A., et al. 2010. Mol. Pharm. 77, 704.