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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).
|Storage||Store at +4°C|
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.
|Solvent||Max Conc. mg/mL||Max Conc. mM|
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|
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
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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
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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.
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Cell Cycle & DNA Damage Repair Poster
In normal cells, each stage of the cell cycle is tightly regulated, however in cancer cells many genes and proteins that are involved in the regulation of the cell cycle are mutated or over expressed. Adapted from the 2015 Cancer Product Guide, Edition 3, this poster summarizes the stages of the cell cycle and DNA repair. It also highlights strategies for enhancing replicative stress in cancer cells to force mitotic catastrophe and cell death.