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Submit ReviewH2L 5765834
Description: LPA1,3,5 antagonist
Chemical Name: 2,3-Dihydro-2-[3-(4-nitrophenoxy)phenyl]-1,3-dioxo-1H-isoindole-5-carboxylic acid
Purity: ≥99% (HPLC)
Biological Activity for H2L 5765834
H2L 5765834 is an 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.
Compound Libraries for H2L 5765834
H2L 5765834 is also offered as part of the Tocriscreen 2.0 Max. Find out more about compound libraries available from Tocris.
Technical Data for H2L 5765834
| M. Wt | 404.33 |
| Formula | C21H12N2O7 |
| Storage | Store at +4°C |
| Purity | ≥99% (HPLC) |
| CAS Number | 420841-84-5 |
| PubChem ID | 1365686 |
| InChI Key | HFYPTENHTPNXGP-UHFFFAOYSA-N |
| Smiles | O=C2N(C3=CC=CC(OC4=CC=C([N+]([O-])=O)C=C4)=C3)C(C1=CC(C(O)=O)=CC=C12)=O |
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.
Product Datasheets for H2L 5765834
References for H2L 5765834
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
2 Citations 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
Travis J et al (2023) Prostate cancer cell-platelet bidirectional signaling promotes calcium mobilization, invasion and apoptotic resistance via distinct receptor-ligand pairs. Sci Rep 13 2864 PMID: 36806315
Reviews for H2L 5765834
Average Rating: 5 (Based on 1 Review.)
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H2L 5765834 inhibits LPA induced COX-2 expression in osteosarcoma cells.
By
Christopher Trummer on 10/23/2018
Assay Type: In Vitro
Species: Human
Cell Line/Tissue: Osteosarcoma
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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