Biological Activity
Potent LPA1 antagonist (IC50 = 25 nM). Exhibits >1,200-fold selectivity for LPA1 over LPA3. Attenuates NHLF human lung fibroblast cell proliferation and contraction in vitro. Also reduces plasma histamine levels in mouse LPA-challenge model. Orally bioavailable.
Technical Data
| M. Wt | 482.53 |
| Formula | C28H26N4O4 |
| Storage | Store at -20°C |
| Purity | ≥98% (HPLC) |
| CAS Number | 1396006-71-5 |
| PubChem ID | 71265339 |
| InChI Key | PXQUHYSYFWQRMF-LJQANCHMSA-N |
| Smiles | CC1=C(NC(O[C@H](C)C2=CC=CC=C2)=O)N(C3=CC=C(C4=CC=C(C5(CC5)C(O)=O)C=C4)C=C3)N=N1 |
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 | 48.25 | 100 | |
| ethanol | 9.65 | 20 |
Preparing Stock Solutions
The following data is based on the product molecular weight 482.53. 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 | 2.07 mL | 10.36 mL | 20.72 mL |
| 5 mM | 0.41 mL | 2.07 mL | 4.14 mL |
| 10 mM | 0.21 mL | 1.04 mL | 2.07 mL |
| 50 mM | 0.04 mL | 0.21 mL | 0.41 mL |
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Product Datasheets
References
References are publications that support the products' biological activity.
Qian et al (2012) Discovery of highly selective and orally active lysophosphatidic acid receptor-1 antagonists with potent activity on human lung fibroblasts. J.Med.Chem. 55 7920 PMID: 22894757
Keywords: Ro 6842262, supplier, Ro6842262, potent, LPA1, lysophosphatidic, acid, receptor-1, antagonists, idiopathic, pulmonary, fibrosis, IPF, Lysophosphatidic, Acid, Receptors, Lysophosphatidic, Acid, Receptors, Tocris Bioscience
