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Submit ReviewAR-C 66096 tetrasodium salt
Description: Potent and selective P2Y12 antagonist
Alternative Names: FPL 66096,ARL 66096
Chemical Name: 2-(Propylthio)adenosine-5'-O-(β,γ-difluoromethylene)triphosphate tetrasodium salt
Purity: ≥98% (HPLC)
Biological Activity for AR-C 66096 tetrasodium salt
AR-C 66096 tetrasodium salt is a potent and selective P2Y12 receptor antagonist. Blocks ADP-induced inhibition of adenylyl cyclase in vitro (pKB =7.6) and inhibits ADP-induced aggregation of washed human platelets (pIC50 = 8.16).
Licensing Information
Sold for research purposes under agreement from AstraZeneca
Technical Data for AR-C 66096 tetrasodium salt
| M. Wt | 703.26 |
| Formula | C14H18F2N5Na4O12P3S |
| Storage | Store at -20°C |
| Purity | ≥98% (HPLC) |
| CAS Number | 145782-74-7 |
| PubChem ID | 90488830 |
| InChI Key | IETVOLFQZIGNAQ-HVYRMSERSA-J |
| Smiles | [Na+].[Na+].[Na+].[Na+].CCCSC1=NC(N)=C2N=CN([C@@H]3O[C@H](COP([O-])(=O)OP([O-])(=O)C(F)(F)P([O-])([O-])=O)[C@@H](O)[C@H]3O)C2=N1 |
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.
Product Datasheets for AR-C 66096 tetrasodium salt
References for AR-C 66096 tetrasodium salt
References are publications that support the biological activity of the product.
Humphries et al (1994) FPL 66096: a novel, highly potent and selective antagonist at human platelet P2T-purinoceptors. Br.J.Pharmacol. 113 1057 PMID: 7858849
Ingall et al (1999) Antagonists of the platelet P receptor: a novel approach to antithrombotic therapy. J.Med.Chem. 42 213 PMID: 9925726
Simon et al (2001) Activity of adenosine diphosphates and triphosphates on a P2YT-type receptor in brain capillary endothelial cells. Br.J.Pharmacol. 132 173 PMID: 11156575
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7 Citations for AR-C 66096 tetrasodium salt
Citations are publications that use Tocris products. Selected citations for AR-C 66096 tetrasodium salt include:
Zhang et al (2014) Agonist-bound structure of the human P2Y12 receptor. Purinergic Signal 509 119 PMID: 24784220
Gao et al (2013) The role of P2Y(14) and other P2Y receptors in degranulation of human LAD2 mast cells. Cell Commun Signal 9 31 PMID: 22825617
Helms et al (2013) Mechanisms of hemolysis-associated platelet activation. J Thromb Haemost 11 2148 PMID: 24119131
Pinheiro et al (2013) Bradykinin-induced Ca2+ signaling in human subcutaneous fibroblasts involves ATP release via hemichannels leading to P2Y12 receptors activation. Cell Commun Signal 11 70 PMID: 24047499
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
Lu et al (2018) The P2Y12 Receptor Antagonist Ticagrelor Reduces Lysosomal pH and Autofluorescence in Retinal Pigmented Epithelial Cells From the ABCA4-/- Mouse Model of Retinal Degeneration. Front Pharmacol 9 242 PMID: 29725296
Chan et al (2018) Not all light transmission aggregation assays are created equal: qualitative differences between light transmission and 96-well plate aggregometry. Platelets 29 686 PMID: 29715047
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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.