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Potent LPA1 antagonist (IC50 = 25 nM). Exhibits >1,200-fold selectivity for LPA1 over LPA3. Attenuates NHLF human lung fibroblast cell proliferation and contraction in vitro. Also reduces plasma histamine levels in mouse LPA-challenge model. Orally bioavailable.
|Storage||Store at -20°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 482.53. 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||2.07 mL||10.36 mL||20.72 mL|
|5 mM||0.41 mL||2.07 mL||4.14 mL|
|10 mM||0.21 mL||1.04 mL||2.07 mL|
|50 mM||0.04 mL||0.21 mL||0.41 mL|
References are publications that support the biological activity of the product.
Qian et al (2012) Discovery of highly selective and orally active lysophosphatidic acid receptor-1 antagonists with potent activity on human lung fibroblasts. J.Med.Chem. 55 7920 PMID: 22894757
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Keywords: Ro 6842262, Ro 6842262 supplier, Ro6842262, potent, LPA1, lysophosphatidic, acid, receptor-1, antagonists, idiopathic, pulmonary, fibrosis, IPF, Lysophosphatidic, Acid, Receptors, 5913, Tocris Bioscience
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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 (Ro 6842262 ) 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 more 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.