AR-C 66096 tetrasodium salt
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).
Sold for research purposes under agreement from AstraZeneca
|Storage||Store at -20°C|
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
All Tocris products are intended for laboratory research use only.
|Solubility||Soluble in water (supplied pre-dissolved at a concentration of 10mM)|
Preparing Stock Solutions
The following data is based on the product molecular weight 703.26. Batch specific molecular weights may vary from batch to batch due to solvent 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||1.42 mL||7.11 mL||14.22 mL|
|5 mM||0.28 mL||1.42 mL||2.84 mL|
|10 mM||0.14 mL||0.71 mL||1.42 mL|
|50 mM||0.03 mL||0.14 mL||0.28 mL|
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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5 Citations for AR-C 66096 tetrasodium salt
Citations are publications that use Tocris products. Selected citations for AR-C 66096 tetrasodium salt include:
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
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
Zhang et al (2014) Agonist-bound structure of the human P2Y12 receptor. Purinergic Signal 509 119 PMID: 24784220
Do you know of a great paper that uses AR-C 66096 tetrasodium salt from Tocris? Please let us know.
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