PSB 0739

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Cat.No. 3983 - PSB 0739 | C26H17N3Na2O8S2 | CAS No. 1052087-90-7
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)
Datasheet
Citations (5)
Reviews (1)
Literature

Biological Activity

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

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

Solvent Max Conc. mg/mL Max Conc. mM
Solubility
water 15.24 25

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

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Product Datasheets

Certificate of Analysis / Product Datasheet
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References

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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5 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

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

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

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

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

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P2Y12 blocker: Average, publishable, might use again.
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.


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