Ro 6842262

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Cat.No. 5913 - Ro 6842262 | C28H26N4O4 | CAS No. 1396006-71-5
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)
Datasheet
Citations
Literature

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

Safety Datasheet

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


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