PSB 0739
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Description: Highly potent P2Y12 antagonist
Chemical Name: 1-Amino-9,10-dihydro-9,10-dioxo-4-[[4-(phenylamino)-3-sulfophenyl]amino]-2-anthracenesulfonic acid sodium salt
Purity: ≥95%
Biological Activity
PSB 0739 is a highly potent P2Y12 receptor antagonist (Ki = 24.9 nM). Unlike clopidogrel (Cat. No. 2490), does not require bioactivation.Technical Data
M.Wt:
609.54
Formula:
C26H17N3Na2O8S2
Solubility:
Soluble to 25 mM in water
Purity:
≥95%
Storage:
Desiccate at RT
CAS No:
1052087-90-7
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.
Additional Information
Licensing Caveats:
Sold with the permission of the University of Bonn.
Background References
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Microglial Kv1.3 Channels and P2Y12 Receptors Differentially Regulate Cytokine and Chemokine Release from Brain Slices of Young Adult and Aged Mice.
Charolidi N, Schilling T, Eder C
PLoS ONE, 2015;10(5):e0128463. -
Infection of microglia with Porphyromonas gingivalis promotes cell migration and an inflammatory response through the gingipain-mediated activation of protease-activated receptor-2 in mice
Y Liu, Z Wu, Y Nakanishi, J Ni, Y Hayashi, F Takayama, Y Zhou, T Kadawaki, H Nakanishi
Sci Rep, 2017;7(1):11759. -
Interaction of new, very potent non-nucleotide antagonists with Arg256 of the human platelet P2Y12 receptor.
Hoffmann et al.
J.Pharmacol.Exp.Ther., 2009;331:648 -
High-affinity, non-nucleotide-derived competitive antagonists of platelet P2Y12 receptors.
Baqi et al.
J.Med.Chem., 2009;52:3784 -
Development of a comprehensive set of P2 receptor pharmacological research compounds.
Felix et al.
Purinerg.Sig., 2011;8:101
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Citations for PSB 0739
The citations listed below are publications that use Tocris products. Selected citations for PSB 0739 include:
15 Citations: Showing 1 - 10
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Microglia modulate blood flow, neurovascular coupling, and hypoperfusion via purinergic actions.
Authors: Domokos Et al.
J Exp Med 2022;219
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The dualistic role of the purinergic P2Y12-receptor in an in vivo model of Parkinson's disease: Signalling pathway and novel therapeutic targets.
Authors: Tibor Et al.
Pharmacol Res 2022;176:106045
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TREM2 regulates purinergic receptor-mediated calcium signaling and motility in human iPSC-derived microglia.
Authors: Stefano L Et al.
Elife 2022;11
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Involvement of P2Y12 receptors in a nitroglycerin-induced model of migraine in male mice.
Authors: Mária Et al.
Br J Pharmacol 2021;178:4626-4645
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Microglia Monitor and Protect Neuronal Function Through Specialized Somatic Purinergic Junctions.
Authors: Cserép Et al.
Science 2020;367:528
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Prevention of P2 Receptor-Dependent Thrombocyte Activation by Pore-Forming Bacterial Toxins Improves Outcome in A Murine Model of Urosepsis.
Authors: Anne-Mette Et al.
Int J Mol Sci 2020;21
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Antiplatelet Drug Ticagrelor Enhances Chemotherapeutic Efficacy by Targeting the Novel P2Y12-AKT Pathway in Pancreatic Cancer Cells.
Authors: Alice Et al.
Cancers (Basel) 2020;12
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Resident Macrophages Cloak Tissue Microlesions to Prevent Neutrophil-Driven Inflammatory Damage.
Authors: Uderhardt Et al.
Cell 2019;177:541
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Microglial Ramification, Surveillance, and Interleukin-1β Release Are Regulated by the Two-Pore Domain K+ Channel THIK-1.
Authors: Madry Et al.
Neuron 2018;97:299
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iPSC-Derived Human Microglia-like Cells to Study Neurological Diseases.
Authors: Abud Et al.
Neuron 2017;94:278
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Protease-activated receptor-4 and P2Y12 Dimerize, Co-Internalize and Activate Akt Signaling via Endosomal Recruitment of β-arrestin.
Authors: Smith Et al.
J Biol Chem 2017;
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Diurnal dynamic behavior of microglia in response to infected bacteria through the UDP-P2Y6 receptor system
Authors: Takayama Et al.
Scientific Reports 2016;6:30006
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Inverse agonism at the P2Y12 receptor and ENT1 transporter blockade contribute to platelet inhibition by ticagrelor.
Authors: Aungraheeta Et al.
Blood 2016;128:2717
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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.
Authors: Nishimura Et al.
PLoS Pathog 2015;11:e1005184
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Nucleolin down-regulation is involved in ADP-induced cell cycle arrest in S phase and cell apoptosis in vascular endothelial cells.
Authors: Wang Et al.
PLoS One 2014;9:e110101
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