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Submit ReviewVU 0364739 hydrochloride
Description: Potent and selective PLD2 inhibitor
Chemical Name: N-[2-[1-(3-Fluorophenyl)-4-oxo-1,3,8-triazaspiro[4.5]dec-8-yl]ethyl]-2-naphthalenecarboxamide
Purity: ≥98% (HPLC)
Biological Activity for VU 0364739 hydrochloride
VU 0364739 hydrochloride is a potent and selective phospholipase D2 (PLD2) inhibitor (IC50 = 20 nM); displays 75-fold selectivity against PLD1 (IC50 = 1500 nM).
Compound Libraries for VU 0364739 hydrochloride
VU 0364739 hydrochloride is also offered as part of the Tocriscreen 2.0 Max. Find out more about compound libraries available from Tocris.
Technical Data for VU 0364739 hydrochloride
| M. Wt | 482.98 |
| Formula | C26H27FN4O2.HCl |
| Storage | Desiccate at RT |
| Purity | ≥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 |
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.
Solubility Data for VU 0364739 hydrochloride
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| DMSO | 48.3 | 100 |
Preparing Stock Solutions for VU 0364739 hydrochloride
The following data is based on the product molecular weight 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.
| Concentration / Solvent Volume / Mass | 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 |
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Product Datasheets for VU 0364739 hydrochloride
References for VU 0364739 hydrochloride
References are publications that support the biological activity of the product.
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
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Keywords: VU 0364739 hydrochloride, VU 0364739 hydrochloride supplier, VU0364739, hydrochloride, phospholipases, d1, d2, potent, selective, inhibitors, inhibits, pld2, Phospholipases, 4171, Tocris Bioscience
10 Citations for VU 0364739 hydrochloride
Citations are publications that use Tocris products. Selected citations for VU 0364739 hydrochloride include:
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
Do you know of a great paper that uses VU 0364739 hydrochloride from Tocris? Please let us know.
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