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Submit ReviewAR-C 69931 tetrasodium salt
Description: Highly potent P2Y12 antagonist
Alternative Names: Cangrelor tetrasodium salt
Chemical Name: N-[2-(Methylthio)ethyl]-2-[(3,3,3-trifluoropropyl)thio]adenosine-5'-O-(β,γ-dichloromethylene)triphosphate tetrasodium salt
Purity: ≥98% (HPLC)
Biological Activity for AR-C 69931 tetrasodium salt
AR-C 69931 tetrasodium salt is a highly potent P2Y12 antagonist (IC50 = 0.4 nM). Inhibits ADP-induced human platelet aggregation ex vivo. Reduces thrombus weight and delays thrombus formation in a model of carotid artery thrombosis in vivo.
Technical Data for AR-C 69931 tetrasodium salt
| M. Wt | 864.29 |
| Formula | C17H21Cl2F3N5Na4O12P3S2 |
| Storage | Store at -20°C |
| Purity | ≥98% (HPLC) |
| CAS Number | 163706-36-3 |
| PubChem ID | 10260031 |
| InChI Key | COWWROCHWNGJHQ-OPKBHZIBSA-J |
| Smiles | O[C@@H]1[C@H](O)[C@@H](N2C3=NC(SCCC(F)(F)F)=NC(NCCSC)=C3N=C2)O[C@H]1COP(OP(C(Cl)(Cl)P(O[Na])(O[Na])=O)(O[Na])=O)(O[Na])=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 AR-C 69931 tetrasodium salt
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| water | 86.43 | 100 |
Preparing Stock Solutions for AR-C 69931 tetrasodium salt
The following data is based on the product molecular weight 864.29. 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 |
|---|---|---|---|
| 1 mM | 1.16 mL | 5.79 mL | 11.57 mL |
| 5 mM | 0.23 mL | 1.16 mL | 2.31 mL |
| 10 mM | 0.12 mL | 0.58 mL | 1.16 mL |
| 50 mM | 0.02 mL | 0.12 mL | 0.23 mL |
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Product Datasheets for AR-C 69931 tetrasodium salt
References for AR-C 69931 tetrasodium salt
References are publications that support the biological activity of the product.
Huang et al (2000) Prevention of arterial thrombosis by intravenously administered platelet P2T receptor antagonist AR-C69931MX in a canine model. J.Pharmacol.Exp.Ther. 295 492 PMID: 11046080
Ingall et al (1999) Antagonists of the platelet P2T receptor: a novel approach to antithrombotic therapy. J.Med.Chem. 42 213 PMID: 9925726
Srinivasan et al (2009) The P2Y12 antagonists, 2-methylthioadenosine 5'-monophosphate triethylammonium salt and cangrelor (ARC69931MX), can inhibit human platelet aggregation through a Gi-independent increase in cAMP levels. J.Biol.Chem. 284 16108 PMID: 19346255
If you know of a relevant reference for AR-C 69931 tetrasodium salt, please let us know.
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6 Citations for AR-C 69931 tetrasodium salt
Citations are publications that use Tocris products. Selected citations for AR-C 69931 tetrasodium salt include:
Sally et al (2019) Promiscuous G-Protein-Coupled Receptor Inhibition of Transient Receptor Potential Melastatin 3 Ion Channels by Gβγ Subunits. J Neurosci 39 7840-7852 PMID: 31451581
Chris et al (2020) Neuronal hyperexcitability is a DLK-dependent trigger of herpes simplex virus reactivation that can be induced by IL-1. Elife 9 PMID: 33350386
Vivek et al (2020) Three-dimensional growth of breast cancer cells potentiates the anti-tumor effects of unacylated ghrelin and AZP-531. Elife 9 PMID: 32667883
Yu et al (2020) Cancer associated fibroblast FAK regulates malignant cell metabolism. Nat Commun 11 1290 PMID: 32157087
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
H C et al (2000) Activation of group II metabotropic glutamate receptors induces long-term depression of synaptic transmission in the rat amygdala. J Neurosci 20 9017-24 PMID: 11124977
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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.