Antagonist of the lysophosphatidic acid receptors LPA1, LPA5 and LPA3 (IC50 values are 94, 463 and 752 nM respectively). Exhibits no effect at LPA2 or LPA4 receptors.
|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 404.33. 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||2.47 mL||12.37 mL||24.73 mL|
|5 mM||0.49 mL||2.47 mL||4.95 mL|
|10 mM||0.25 mL||1.24 mL||2.47 mL|
|50 mM||0.05 mL||0.25 mL||0.49 mL|
References are publications that support the biological activity of the product.
Williams et al (2009) Unique ligand selectivity of the GPR92/LPA5 lysophosphatidate receptor indicates role in human platelet activation. J.Biol.Chem. 284 17304 PMID: 19366702
Fells et al (2010) 2D binary QSAR modeling of LPA3 receptor antagonism. J.Mol.Graph Model. 28 828 PMID: 20356772
Tigyi (2010) Aiming drug discovery at lysophosphatidic acid targets. Br.J.Pharmacol. 161 241 PMID: 20735414
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Keywords: H2L 5765834, H2L 5765834 supplier, H2L5765834, lysophosphatidic, acid, receptors, LPA1, LPA3, LPA5, antagonists, Lysophosphatidic, Acid, Receptors, 4870, Tocris Bioscience
1 Citation for H2L 5765834
Citations are publications that use Tocris products. Selected citations for H2L 5765834 include:
Kittaka et al (2017) Lysophosphatidic acid-induced itch is mediated by signalling of LPA5 receptor, phospholipase D and TRPA1/TRPV1. J Physiol 595 2681 PMID: 28176353
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MG-63 cells were treated with LPA (10 µM) alone or in combination with C3 (20 µM), PTX (Pertussis Toxin, 400 ng/ml) or H2L 5765834 (20 µM) for 3 h to follow COX-2 expression using Western blot. H2L inhibited COX-2 expression induced by LPA.
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