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Highly potent P2Y12 receptor antagonist (Ki = 24.9 nM). Unlike clopidogrel (Cat. No. 2490), does not require bioactivation.
Sold with the permission of the University of Bonn.
|Storage||Desiccate at RT|
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.
|Solvent||Max Conc. mg/mL||Max Conc. mM|
Preparing Stock Solutions
The following data is based on the product molecular weight 609.54. 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|
|0.25 mM||6.56 mL||32.81 mL||65.62 mL|
|1.25 mM||1.31 mL||6.56 mL||13.12 mL|
|2.5 mM||0.66 mL||3.28 mL||6.56 mL|
|12.5 mM||0.13 mL||0.66 mL||1.31 mL|
References are publications that support the biological activity of the product.
Hoffmann et al (2009) Interaction of new, very potent non-nucleotide antagonists with Arg256 of the human platelet P2Y12 receptor. J.Pharmacol.Exp.Ther. 331 648 PMID: 19690189
Baqi et al (2009) High-affinity, non-nucleotide-derived competitive antagonists of platelet P2Y12 receptors. J.Med.Chem. 52 3784 PMID: 19463000
Felix et al (2011) Development of a comprehensive set of P2 receptor pharmacological research compounds. Purinerg.Sig. 8 101 PMID: 22052555
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Keywords: PSB 0739, PSB 0739 supplier, PSB0739, potent, selective, p2y12, purine, receptors, antagonist, purinoceptors, purinergic, Purinergic, P2Y, Receptors, 3983, Tocris Bioscience
9 Citations for PSB 0739
Citations are publications that use Tocris products. Selected citations for PSB 0739 include:
Wang et al (2014) Nucleolin down-regulation is involved in ADP-induced cell cycle arrest in S phase and cell apoptosis in vascular endothelial cells. PLoS One 9 e110101 PMID: 25290311
Takayama et al (2016) Diurnal dynamic behavior of microglia in response to infected bacteria through the UDP-P2Y6 receptor system Scientific Reports 6 30006 PMID: 27445174
Cserép et al (2020) Microglia Monitor and Protect Neuronal Function Through Specialized Somatic Purinergic Junctions. Science 367 528 PMID: 31831638
Smith et al (2017) Protease-activated receptor-4 and P2Y12 Dimerize, Co-Internalize and Activate Akt Signaling via Endosomal Recruitment of β-arrestin. J Biol Chem PMID: 28652403
Aungraheeta et al (2016) Inverse agonism at the P2Y12 receptor and ENT1 transporter blockade contribute to platelet inhibition by ticagrelor. Blood 128 2717 PMID: 27694321
Uderhardt et al (2019) Resident Macrophages Cloak Tissue Microlesions to Prevent Neutrophil-Driven Inflammatory Damage. Cell 177 541 PMID: 30955887
Nishimura et al (2015) The Suramin Derivative NF449 Interacts with the 5-fold Vertex of the Enterovirus A71 Capsid to Prevent Virus Attachment to PSGL-1 and Heparan Sulfate. PLoS Pathog 11 e1005184 PMID: 26430888
Madry et al (2018) Microglial Ramification, Surveillance, and Interleukin-1β Release Are Regulated by the Two-Pore Domain K+ Channel THIK-1. Neuron 97 299 PMID: 29290552
Abud et al (2017) iPSC-Derived Human Microglia-like Cells to Study Neurological Diseases. Neuron 94 278 PMID: 28426964
Do you know of a great paper that uses PSB 0739 from Tocris? Please let us know.
Reviews for PSB 0739
Average Rating: 4 (Based on 2 Reviews.)
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H20; dilution 10 μM
Used to block P2Y12 in acute brain slices. Monitored was the motility of microglia. No significant effect was found.
Literature in this Area
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