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Submit ReviewRo 6842262
说明： Potent LPA1 antagonist
化学名： 1-[4'-[4-Methyl-5-[[[(1R)-1-phenylethoxy]carbonylamino]-1H-1,2,3-triazol-1-yl][1,1'-biphenyl]-4-yl]cyclopropanecarboxylic acid
纯度： ≥98% (HPLC)
生物活性 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.
化合物库 for Ro 6842262
Ro 6842262 is also offered as part of the Tocriscreen 2.0 Max. 了解 Tocris 化合物库的更多信息。
技术数据 for Ro 6842262
| 分子量 | 482.53 |
| 公式 | C28H26N4O4 |
| 储存 | Store at -20°C |
| 纯度 | ≥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 |
上方提供的技术数据仅供参考。批次相关数据请参见分析证书。
Tocris products are intended for laboratory research use only, unless stated otherwise.
溶解性数据 for Ro 6842262
| 溶剂 | 最高浓度 mg/mL | 最高浓度 mM | |
|---|---|---|---|
| 溶解性 | |||
| DMSO | 48.25 | 100 | |
| ethanol | 9.65 | 20 |
制备储备液 for Ro 6842262
以下数据基于产品分子量 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.
| 浓度/溶剂体积/质量 | 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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产品说明书 for Ro 6842262
参考文献 for Ro 6842262
参考文献是支持产品生物活性的出版物。
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
If you know of a relevant reference for Ro 6842262, please let us know.
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关键词: Ro 6842262, Ro 6842262 supplier, Ro6842262, potent, LPA1, lysophosphatidic, acid, receptor-1, antagonists, idiopathic, pulmonary, fibrosis, IPF, Lysophosphatidic, Acid, Receptors, 5913, Tocris Bioscience
1 篇 Ro 6842262 的引用文献
引用文献是使用了 Tocris 产品的出版物。 Ro 6842262 的部分引用包括：
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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Ro 6842262 的评论
平均评分: 4 (Based on 1 Review.)
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Works as a negative control to LPA-induced suppression.
By
Anonymous on 11/18/2018
分析类型： In Vitro
种属： Mouse
细胞系/组织： 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.
该领域的文献
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*请注意，Tocris 仅会向正规科研企业/机构地址发送文献。
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In normal cells, each stage of the cell cycle is tightly regulated, however in cancer cells many genes and proteins that are involved in the regulation of the cell cycle are mutated or over expressed. This poster summarizes the stages of the cell cycle and DNA repair. It also highlights strategies for enhancing replicative stress in cancer cells to force mitotic catastrophe and cell death.