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Cat.No. 4878 - H2L5186303 | C26H20N2O8 | CAS No. 139262-76-3
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 (2)
Reviews (1)

Biological Activity

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

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

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

Preparing Stock Solutions

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.

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 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

2 Citations for H2L5186303

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

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

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

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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