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Description: Potent and selective LPA2 receptor antagonist
Chemical Name: (Z,Z)-4,4'-[1,3-Phenylenebis(oxy-4,1-phenyleneimino)]bis[4-oxo-2-butenoic acid
Purity: ≥98% (HPLC)
Citations (6)
Reviews (1)
Literature (2)

Biological Activity for H2L5186303

H2L5186303 is a potent and selective lysophosphatidic acid 2 (LPA2) receptor antagonist (IC50 values are 8.9, 1230 and 27354 nM for LPA2, LPA3 and LPA1 receptors respectively, in a LPA-elicited calcium mobilization assay).

Technical Data for H2L5186303

M. Wt 488.45
Formula C26H20N2O8
Storage Store at +4°C
Purity ≥98% (HPLC)
CAS Number 139262-76-3
PubChem ID 90488981
Smiles O=C(/C=C\C(O)=O)NC(C=C3)=CC=C3OC1=CC(OC2=CC=C(NC(/C=C\C(O)=O)=O)C=C2)=CC=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.

Solubility Data for H2L5186303

Solvent Max Conc. mg/mL Max Conc. mM
DMSO 48.84 100

Preparing Stock Solutions for H2L5186303

The following data is based on the product molecular weight 488.45. 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.

Select a batch to recalculate based on the batch molecular weight:
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 2.05 mL 10.24 mL 20.47 mL
5 mM 0.41 mL 2.05 mL 4.09 mL
10 mM 0.2 mL 1.02 mL 2.05 mL
50 mM 0.04 mL 0.2 mL 0.41 mL

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References for H2L5186303

References are publications that support the biological activity of the product.

Fells et al (2008) Identification of non-lipid LPA3 antagonists by virtual screening. Bioorg.Med.Chem. 16 6207 PMID: 18467108

Fells et al (2009) Structure-based drug design identifies novel LPA3 antagonists. Bioorg.Med.Chem. 17 7457 PMID: 19800804

If you know of a relevant reference for H2L5186303, please let us know.

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Keywords: H2L5186303, H2L5186303 supplier, lysophosphatidic, acid, 2, receptors, LPA2, antagonists, Lysophosphatidic, Acid, Receptors, 4878, Tocris Bioscience

6 Citations for H2L5186303

Citations are publications that use Tocris products. Selected citations for H2L5186303 include:

Volden et al (2016) Mammary Adipose Tissue-Derived Lysophospholipids Promote Estrogen Receptor-Negative Mammary Epithelial Cell Proliferation. Cancer Prev Res (Phila) 9 367 PMID: 26862086

Robert et al (2023) The lysophosphatidic acid-regulated signal transduction network in ovarian cancer cells and its role in actomyosin dynamics, cell migration and entosis. Theranostics 13 1921-1948 PMID: 37064875

Yoshihiro et al (2021) Lysophosphatidic acid induces thrombospondin-1 production in primary cultured rat cortical astrocytes. J Neurochem 158 849-864 PMID: 33118159

Wu et al (2015) Mechanosensitive PPAP2B Regulates Endothelial Responses to Atherorelevant Hemodynamic Forces. PLoS One 117 e41 PMID: 26034042

Do you know of a great paper that uses H2L5186303 from Tocris? Please let us know.

Reviews for H2L5186303

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Works as a negative control for LPA effects in culture..
By Anonymous on 11/18/2018
Assay Type: In Vivo
Species: Mouse
Cell Line/Tissue: primary mammary epithelium

Mouse Mammary epithelial cells were used in a standard mammosphere generating assay in a serum-free (B27 supplement), non-adherent condition. LPA or LPA antagonist (H2L5186303) were added to media and the number of spheres were counted after 6 days of culture. Results showed that 10 uM of the antagonist ameliorated most of the LPA-induced suppression, but did not fully neutralize LPA effects. Of two tested LPA inhibitors (products #4878, #5913), this was less effective by a small margin.

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Literature in this Area

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