P2X receptors, which are ligand-gated ion channels, are freely permeable to the three most important physiological cations: sodium, potassium, and calcium. P2X receptors open in the presence of extracellular adenosine triphosphate (ATP) and play an important role in regulating the homeostasis of a range of organisms. P2X receptors are generally classified as ligand-gated cation channels because most of their physiological effects result from the inward flow of cations across the cell surface membrane. The ATP binding site of P2X receptors resides at the interface of neighboring subunits of the multimeric receptor complex.
P2 Receptor
Other Neuronal Signaling Inhibitors
Isoform-selective Products
| Cat.No. | Product Name | Information | Product Use Citations | Product Validations |
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| S4079 | Ticagrelor | Ticagrelor (AZD6140, AR-C 126532XX) is the first reversibly binding oral P2Y12 receptor antagonist with Ki of 2 nM. |
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| S7705 | A-438079 Hydrochloride | A-438079 HCl is a potent, and selective P2X7 receptor antagonist with pIC50 of 6.9. |
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| E1128 | BzATP triethylammonium salt | BzATP triethylammonium salt acts as a P2X receptor agonist with pEC50s of 8.74, 5.26, 7.10, 7.50, 6.19, 6.31, 5.33 for P2X1, P2X2, P2X3, P2X2/3, P2X4 and P2X7, respectively, also is potent at P2X7 receptors with EC50s of 3.6 μM and 285 μM for rat P2X7 and mouse P2X7, respectively. | ||
| S1415 | Clopidogrel (SR-25990C) Bisulfate | Clopidogrel (SR-25990C) Bisulfate is an oral, thienopyridine class antiplatelet agent. |
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| S8725 | A-804598 | A-804598 is a selective P2X7R antagonist with high affinity at rat (IC50 = 10 nM), mouse (IC50 = 9 nM) and human (IC50 = 11 nM) P2X7 receptors. |
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| S3737 | Cangrelor Tetrasodium | Cangrelor (AR-C69931MX) is a potent, competitive P2Y12 receptor inhibitor that is administered by intravenous infusion and rapidly achieves near complete inhibition of ADP-induced platelet aggregation. |
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| S1258 | Prasugrel | Prasugrel (Effient, Efient, Prasita,CS-747, LY640315,PCR 4099) is a thienopyridine ADP receptor (P2Y12) antagonist, used for the reduction of thrombotic cardiovascular events. |
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| S2855 | MRS 2578 | MRS2578 is a potent P2Y6 receptor antagonist with an IC50 of 37 nM, and exhibits insignificant activity at P2Y1, P2Y2, P2Y4, and P2Y11 receptors. |
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| S0826 | A-740003 | A-740003 is a potent, selective and competitive antagonist of P2X7 receptor with IC50 of 18 nM and 40 nM for rat and human P2X7 receptors, respectively. This compound potently blocks agonist-evoked IL-1β release and pore formation with IC50 of 156 nM and 92 nM in differentiated human THP-1 cells. |
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| S4637 | Prasugrel Hydrochloride | Prasugrel hydrochloride (Prasugrel HCl, LY640315, PCR 4099 Hydrochloride) is a piperazine derivative and platelet aggregation inhibitor that is used to prevent thrombosis in patients with acute coronary syndrome. |
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