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Submit ReviewH2L5186303 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).
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.
溶剂 | 最高浓度 mg/mL | 最高浓度 mM | |
---|---|---|---|
溶解性 | |||
DMSO | 48.84 | 100 |
以下数据基于产品分子量 488.45。 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 | 2.05 mL | 10.24 mL | 20.47 mL |
5 mM | 0.41 mL | 2.05 mL | 4.09 mL |
10 mM | 0.2 mL | 1.02 mL | 2.05 mL |
50 mM | 0.04 mL | 0.2 mL | 0.41 mL |
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
If you know of a relevant reference for H2L5186303, please let us know.
关键词: H2L5186303, H2L5186303 supplier, lysophosphatidic, acid, 2, receptors, LPA2, antagonists, Lysophosphatidic, Acid, Receptors, 4878, Tocris Bioscience
引用文献是使用了 Tocris 产品的出版物。 H2L5186303 的部分引用包括:
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
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
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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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*请注意,Tocris 仅会向正规科研企业/机构地址发送文献。
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.