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Submit ReviewRo 6842262
Description: Potent LPA1 antagonist
Chemical Name: 1-[4'-[4-Methyl-5-[[[(1R)-1-phenylethoxy]carbonylamino]-1H-1,2,3-triazol-1-yl][1,1'-biphenyl]-4-yl]cyclopropanecarboxylic acid
Purity: ≥98% (HPLC)
Biological Activity for Ro 6842262
Ro 6842262 is a 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.
Compound Libraries for Ro 6842262
Ro 6842262 is also offered as part of the Tocriscreen 2.0 Max. Find out more about compound libraries available from Tocris.
Technical Data for Ro 6842262
| 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.
Tocris products are intended for laboratory research use only, unless stated otherwise.
Solubility Data for Ro 6842262
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| DMSO | 48.25 | 100 | |
| ethanol | 9.65 | 20 |
Preparing Stock Solutions for Ro 6842262
The following data is based on the product molecular weight 482.53. 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 | 2.07 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 for Ro 6842262
References for Ro 6842262
References are publications that support the biological activity of the product.
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
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Keywords: Ro 6842262, Ro 6842262 supplier, Ro6842262, potent, LPA1, lysophosphatidic, acid, receptor-1, antagonists, idiopathic, pulmonary, fibrosis, IPF, Lysophosphatidic, Acid, Receptors, 5913, Tocris Bioscience
1 Citation for Ro 6842262
Citations are publications that use Tocris products. Selected citations for Ro 6842262 include:
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
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Reviews for Ro 6842262
Average Rating: 4 (Based on 1 Review.)
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Works as a negative control to LPA-induced suppression.
By
Anonymous on 11/18/2018
Assay Type: In Vitro
Species: Mouse
Cell Line/Tissue: primary 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 (Ro 6842262 ) 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 more effective by a small margin.
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