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Submit ReviewVU 0364739 hydrochloride is a potent and selective phospholipase D2 (PLD2) inhibitor (IC50 = 20 nM); displays 75-fold selectivity against PLD1 (IC50 = 1500 nM).
VU 0364739 hydrochloride is also offered as part of the Tocriscreen 2.0 Max. 了解 Tocris 化合物库的更多信息。
分子量 | 482.98 |
公式 | C26H27FN4O2.HCl |
储存 | Desiccate at RT |
纯度 | ≥98% (HPLC) |
CAS Number | 1244640-48-9 |
PubChem ID | 46939225 |
InChI Key | RYLAMDMOILNBKN-UHFFFAOYSA-N |
Smiles | O=C(NCCN3CCC(C(NCN4C5=CC(F)=CC=C5)=O)4CC3)C2=CC1=CC=CC=C1C=C2.Cl |
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 | 48.3 | 100 |
以下数据基于产品分子量 482.98。 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 | 10.35 mL | 20.7 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 |
参考文献是支持产品生物活性的出版物。
Lavieri et al (2010) Design, synthesis, and biological evaluation of halogenated N-(2-(4-oxo-1-phenyl-1,3,8-triazaspiro[4.5]decan-8-yl)-ethyl)benzamides: discovery of an isoform-selective small molecule phospholipase D2 inhibitor. J.Med.Chem. 53 6709
If you know of a relevant reference for VU 0364739 hydrochloride, please let us know.
关键词: VU 0364739 hydrochloride, VU 0364739 hydrochloride supplier, VU0364739, hydrochloride, phospholipases, d1, d2, potent, selective, inhibitors, inhibits, pld2, Phospholipases, 4171, Tocris Bioscience
引用文献是使用了 Tocris 产品的出版物。 VU 0364739 hydrochloride 的部分引用包括:
Bich et al (2018) Physiological function of phospholipase D2 in anti-tumor immunity: regulation of CD8+ T lymphocyte proliferation. Sci Rep 8 6283 PMID: 29674728
Lu et al (2018) An Antithrombotic Strategy by Targeting Phospholipase D in Human Platelets. J Clin Med 7 PMID: 30441821
Tove Irene et al (2021) Diacylglycerol kinase and phospholipase D inhibitors alter the cellular lipidome and endosomal sorting towards the Golgi apparatus. Cell Mol Life Sci 78 985-1009 PMID: 32447426
Basiouni et al (2013) The influence of polyunsaturated fatty acids on the phospholipase D isoforms trafficking and activity in mast cells. Autophagy 14 9005 PMID: 23698760
Liu et al (2017) PLD2 regulates microtubule stability and spindle migration in mouse oocytes during meiotic division. PeerJ 5 e3295 PMID: 28533957
Chelakkot et al (2017) Intestinal Epithelial Cell-Specific Deletion of PLD2 Alleviates DSS-Induced Colitis by Regulating Occludin. Sci Rep 7 1573 PMID: 28484281
Krishnan et al (2018) Elevated phospholipase D isoform 1 in Alzheimer's disease patients' hippocampus: Relevance to synaptic dysfunction and memory deficits. Alzheimer Dement (N Y) 4 89 PMID: 29560412
Jiang et al (2016) Phosphatidic Acid Produced by RalA-activated PLD2 Stimulates Caveolae-mediated Endocytosis and Trafficking in Endothelial Cells. J Biol Chem. 291 20729 PMID: 27510034
Martínez-Martínez et al (2014) Phospholipase D2 is involved in the formation of Golgi tubules and ArfGAP1 recruitment. PLoS One 9 e111685 PMID: 25354038
Xiao-Fan et al (2022) Parkin coordinates mitochondrial lipid remodeling to execute mitophagy. EMBO Rep 23 e55191 PMID: 36256516
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