H2L 5765834
Chemical Name: 2,3-Dihydro-2-[3-(4-nitrophenoxy)phenyl]-1,3-dioxo-1H-isoindole-5-carboxylic acid
Purity: ≥99%
Biological Activity
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.Technical Data
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
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Unique ligand selectivity of the GPR92/LPA5 lysophosphatidate receptor indicates role in human platelet activation.
Williams et al.
J.Biol.Chem., 2009;284:17304 -
2D binary QSAR modeling of LPA3 receptor antagonism.
Fells et al.
J.Mol.Graph Model., 2010;28:828 -
Aiming drug discovery at lysophosphatidic acid targets.
Tigyi
Br.J.Pharmacol., 2010;161:241
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Citation for H2L 5765834
The citations listed below are publications that use Tocris products. Selected citations for H2L 5765834 include:
1 Citation: Showing 1 - 1
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Lysophosphatidic acid-induced itch is mediated by signalling of LPA5 receptor, phospholipase D and TRPA1/TRPV1.
Authors: Kittaka Et al.
J Physiol 2017;595:2681
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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.
