Chemical Name: (Z,Z)-4,4'-[1,3-Phenylenebis(oxy-4,1-phenyleneimino)]bis[4-oxo-2-butenoic acid
Biological ActivityPotent 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).
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.
Identification of non-lipid LPA3 antagonists by virtual screening.
Fells et al.
Structure-based drug design identifies novel LPA3 antagonists.
Fells et al.
Citations for H2L5186303
The citations listed below are publications that use Tocris products. Selected citations for H2L5186303 include:
2 Citations: Showing 1 - 2
Mammary Adipose Tissue-Derived Lysophospholipids Promote Estrogen Receptor-Negative Mammary Epithelial Cell Proliferation.
Authors: Volden Et al.
Cancer Prev Res (Phila) 2016;9:367
Mechanosensitive PPAP2B Regulates Endothelial Responses to Atherorelevant Hemodynamic Forces.
Authors: Wu Et al.
PLoS One 2015;117:e41
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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.