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.
Compound Libraries
H2L 5765834 is also offered as part of the Tocriscreen Plus. Find out more about compound libraries available from Tocris.
Technical Data
| 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.
All Tocris products are intended for laboratory research use only.
Solubility Data
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| DMSO | 40.43 | 100 |
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 solvent 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 |
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Product Datasheets
References
References are publications that support the products' biological activity.
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
Keywords: H2L 5765834, supplier, H2L5765834, lysophosphatidic, acid, receptors, LPA1, LPA3, LPA5, antagonists, Lysophosphatidic, Acid, Receptors, Lysophosphatidic, Acid, Receptors, Tocris Bioscience
