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说明： Potent and selective LPA2 receptor antagonist
化学名： (Z,Z)-4,4'-[1,3-Phenylenebis(oxy-4,1-phenyleneimino)]bis[4-oxo-2-butenoic acid
纯度： ≥98% (HPLC)
生物活性 for H2L5186303
H2L5186303 is a potent and selective lysophosphatidic acid 2 (LPA2) receptor antagonist (IC50 values are 8.9, 1230 and 27354 nM for LPA2, LPA3 and LPA1 receptors respectively, in a LPA-elicited calcium mobilization assay).
技术数据 for H2L5186303
| 分子量 | 488.45 |
| 公式 | C26H20N2O8 |
| 储存 | Store at +4°C |
| 纯度 | ≥98% (HPLC) |
| CAS Number | 139262-76-3 |
| PubChem ID | 90488981 |
| InChI Key | HZFPOTBCYPWQSH-DZDAAMPGSA-N |
| Smiles | O=C(/C=C\C(O)=O)NC(C=C3)=CC=C3OC1=CC(OC2=CC=C(NC(/C=C\C(O)=O)=O)C=C2)=CC=C1 |
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.
产品说明书 for H2L5186303
参考文献 for H2L5186303
参考文献是支持产品生物活性的出版物。
Fells et al (2008) Identification of non-lipid LPA3 antagonists by virtual screening. Bioorg.Med.Chem. 16 6207 PMID: 18467108
Fells et al (2009) Structure-based drug design identifies novel LPA3 antagonists. Bioorg.Med.Chem. 17 7457 PMID: 19800804
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关键词: H2L5186303, H2L5186303 supplier, lysophosphatidic, acid, 2, receptors, LPA2, antagonists, Lysophosphatidic, Acid, Receptors, 4878, Tocris Bioscience
6 篇 H2L5186303 的引用文献
引用文献是使用了 Tocris 产品的出版物。 H2L5186303 的部分引用包括：
Paul et al (2020) P130Cas/bcar1 mediates zebrafish caudal vein plexus angiogenesis. Sci Rep 10 15589 PMID: 32973180
Volden et al (2016) Mammary Adipose Tissue-Derived Lysophospholipids Promote Estrogen Receptor-Negative Mammary Epithelial Cell Proliferation. Cancer Prev Res (Phila) 9 367 PMID: 26862086
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
Wu et al (2015) Mechanosensitive PPAP2B Regulates Endothelial Responses to Atherorelevant Hemodynamic Forces. PLoS One 117 e41 PMID: 26034042
Yoshihiro et al (2021) Lysophosphatidic acid induces thrombospondin-1 production in primary cultured rat cortical astrocytes. J Neurochem 158 849-864 PMID: 33118159
Shigeru et al (2022) Lysophosphatidic Acid Promotes the Expansion of Cancer Stem Cells via TRPC3 Channels in Triple-Negative Breast Cancer. Int J Mol Sci 23 PMID: 35216080
H2L5186303 的评论
平均评分: 4 (Based on 1 Review.)
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Works as a negative control for LPA effects in culture..
By
Anonymous on 11/18/2018
分析类型： In Vivo
种属： Mouse
细胞系/组织： primary mammary 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 (H2L5186303) 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 less effective by a small margin.
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