Catalog # Availability Size / Price Qty
H2L5186303 | CAS No. 139262-76-3 | Lysophosphatidic Acid (LPA) Receptor Antagonists
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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

Product Details
Citations (2)
Supplemental Products
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

Soluble to 100 mM in DMSO
Store the unopened product at 2 - 8 °C. Do not use past expiration date.

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.

Background References

  1. Identification of non-lipid LPA3 antagonists by virtual screening.
    Fells et al.
    Bioorg.Med.Chem., 2008;16:6207
  2. Structure-based drug design identifies novel LPA3 antagonists.
    Fells et al.
    Bioorg.Med.Chem., 2009;17:7457

Product Datasheets

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Citations for H2L5186303

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Works as a negative control for LPA effects in culture.
By Anonymous on 11/18/2018
Species: Mouse

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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