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Description: Potent and selective LPA2 receptor antagonist
Chemical Name: (Z,Z)-4,4'-[1,3-Phenylenebis(oxy-4,1-phenyleneimino)]bis[4-oxo-2-butenoic acid
Purity: ≥98% (HPLC)
Biological Activity for H2L5186303
H2L5186303 is a 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).
Technical Data for H2L5186303
| M. Wt | 488.45 |
| Formula | C26H20N2O8 |
| Storage | Store at +4°C |
| Purity | ≥98% (HPLC) |
| CAS Number | 139262-76-3 |
| PubChem ID | 90488981 |
| InChI Key | HZFPOTBCYPWQSH-DZDAAMPGSA-N |
| Smiles | O=C(/C=C\C(O)=O)NC(C=C3)=CC=C3OC1=CC(OC2=CC=C(NC(/C=C\C(O)=O)=O)C=C2)=CC=C1 |
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.
Solubility Data for H2L5186303
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| DMSO | 48.84 | 100 |
Preparing Stock Solutions for H2L5186303
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 |
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Product Datasheets for H2L5186303
References for H2L5186303
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
6 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
Yoshihiro et al (2021) Lysophosphatidic acid induces thrombospondin-1 production in primary cultured rat cortical astrocytes. J Neurochem 158 849-864 PMID: 33118159
Shigeru et al (2022) Lysophosphatidic Acid Promotes the Expansion of Cancer Stem Cells via TRPC3 Channels in Triple-Negative Breast Cancer. Int J Mol Sci 23 PMID: 35216080
Paul et al (2020) P130Cas/bcar1 mediates zebrafish caudal vein plexus angiogenesis. Sci Rep 10 15589 PMID: 32973180
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
Robert et al (2023) The lysophosphatidic acid-regulated signal transduction network in ovarian cancer cells and its role in actomyosin dynamics, cell migration and entosis. Theranostics 13 1921-1948 PMID: 37064875
Do you know of a great paper that uses H2L5186303 from Tocris? Please let us know.
Reviews for H2L5186303
Average Rating: 4 (Based on 1 Review.)
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Works as a negative control for LPA effects in culture..
By
Anonymous on 11/18/2018
Assay Type: In Vivo
Species: Mouse
Cell Line/Tissue: primary mammary epithelium
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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