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Submit ReviewPSB 0739
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% (HPLC)
Biological Activity for PSB 0739
PSB 0739 is a highly potent P2Y12 receptor antagonist (Ki = 24.9 nM). Unlike clopidogrel (Cat. No. 2490), does not require bioactivation.
Licensing Information
Sold with the permission of the University of Bonn.
Technical Data for PSB 0739
| M. Wt | 609.54 |
| Formula | C26H17N3Na2O8S2 |
| Storage | Desiccate at RT |
| Purity | ≥95% (HPLC) |
| CAS Number | 1052087-90-7 |
| PubChem ID | 44583582 |
| InChI Key | QBLLYXXXOJUNCV-UHFFFAOYSA-L |
| Smiles | [Na+].[Na+].NC1=C(C=C(NC2=CC(=C(NC3=CC=CC=C3)C=C2)S([O-])(=O)=O)C2=C1C(=O)C1=CC=CC=C1C2=O)S([O-])(=O)=O |
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 PSB 0739
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| water | 15.24 | 25 |
Preparing Stock Solutions for PSB 0739
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 |
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Product Datasheets for PSB 0739
References for PSB 0739
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
If you know of a relevant reference for PSB 0739, please let us know.
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Keywords: PSB 0739, PSB 0739 supplier, PSB0739, potent, selective, p2y12, purine, receptors, antagonists, purinoceptors, purinergic, antagonises, inhibitors, inhibits, Purinergic, P2Y, Receptors, 3983, Tocris Bioscience
15 Citations for PSB 0739
Citations are publications that use Tocris products. Selected citations for PSB 0739 include:
Alice et al (2020) Antiplatelet Drug Ticagrelor Enhances Chemotherapeutic Efficacy by Targeting the Novel P2Y12-AKT Pathway in Pancreatic Cancer Cells. Cancers (Basel) 12 PMID: 31968611
Anne-Mette et al (2020) Prevention of P2 Receptor-Dependent Thrombocyte Activation by Pore-Forming Bacterial Toxins Improves Outcome in A Murine Model of Urosepsis. Int J Mol Sci 21 PMID: 32781764
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
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
Mária et al (2021) Involvement of P2Y12 receptors in a nitroglycerin-induced model of migraine in male mice. Br J Pharmacol 178 4626-4645 PMID: 34363208
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
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
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
Uderhardt et al (2019) Resident Macrophages Cloak Tissue Microlesions to Prevent Neutrophil-Driven Inflammatory Damage. Cell 177 541 PMID: 30955887
Domokos et al (2022) Microglia modulate blood flow, neurovascular coupling, and hypoperfusion via purinergic actions. J Exp Med 219 PMID: 35201268
Tibor et al (2022) The dualistic role of the purinergic P2Y12-receptor in an in vivo model of Parkinson's disease: Signalling pathway and novel therapeutic targets. Pharmacol Res 176 106045 PMID: 34968684
Stefano L et al (2022) TREM2 regulates purinergic receptor-mediated calcium signaling and motility in human iPSC-derived microglia. Elife 11 PMID: 35191835
Cserép et al (2020) Microglia Monitor and Protect Neuronal Function Through Specialized Somatic Purinergic Junctions. Science 367 528 PMID: 31831638
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
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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Good inhibitor.
By
Anonymous on 06/06/2020
Assay Type: In Vivo
Species: Mouse
Cell Line/Tissue: phagocyte
H20; dilution 10 μM
P2Y12 blocker.
By
Anonymous on 01/30/2018
Assay Type: Ex Vivo
Species: Mouse
Cell Line/Tissue: acute brain slice
Used to block P2Y12 in acute brain slices. Monitored was the motility of microglia. No significant effect was found.
Literature in this Area
Tocris offers the following scientific literature in this area to showcase our products. We invite you to request* your copy today!
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P2X and P2Y Receptors Scientific Review
Written by Kenneth Jacobson, this review provides an overview of the different subtypes and structures of the P2 receptor families, as well as the pharmacological probes used to study them; compounds available from Tocris are listed.