P2 Receptor

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.

Isoform-selective Products

Cat.No. Product Name Information Product Use Citations Product Validations
S4079 Ticagrelor Ticagrelor (AZD6140, AR-C 126532XX) is the first reversibly binding oral P2Y12 receptor antagonist with Ki of 2 nM.
J Immunother Cancer, 2024, 12(11)e009805
Biochemical Pharmacology, 2024, 226:116408
Nature Biomedical Engineering, 2023, 7(11):1404-1418
Verified customer review of Ticagrelor
S7705 A-438079 Hydrochloride A-438079 HCl is a potent, and selective P2X7 receptor antagonist with pIC50 of 6.9.
Redox Biol, 2024, 72:103154
Cells, 2023, 12(23)2696
Biomol Biomed, 2023, 23(5):825-837
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.
Biomedicines, September 16, 2021, 1230
International Journal of Molecular Sciences, July 20, 2023, 11706
Nat Commun, 2025, 16(1):7974
Verified customer review of Clopidogrel (SR-25990C) Bisulfate
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.
Immunobiology, 2025, 230(6):153119
Biol Pharm Bull, 2025, 48(5):657-671
J Cell Physiol, 2022, 10.1002/jcp.30685
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.
J Immunother Cancer, 2024, 12(11)e009805
J Thromb Haemost, 2023, S1538-7836(23)00082-X
Food Funct, 2021, 10.1039/d1fo00531f
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.
Communications Medicine, 2025, 420
Oncology Letters, 2018, 6107-6114
Oncol Lett, 2018, 15(5):6107-6114
S2855 MRS 2578 MRS2578 is a potent P2Y6 receptor antagonist with IC50 of 37 nM, and exhibits insignificant activity at P2Y1, P2Y2, P2Y4,and P2Y11 receptors.
Heliyon, 2023 Dec 13, 10(1):e23632
Ann Med, 2022, 54(1):1616-1626
Sci Rep, 2021, 11(1):15129
E4929 (S)-Clopidogrel (S)-Clopidogrel is an inhibitor of P2Y12 and exerts anticoagulant effects. It is metabolized into an active form that binds to the P2Y12 receptor, blocking ADP and preventing platelet aggregation. It also exhibits anti-inflammatory and antifibrotic properties in chronic kidney disease (CKD) and liver fibrosis.
PLoS One, October 29, 2021, e0259129
Arteriosclerosis, Thrombosis, and Vascular Biology, November 24, 2020, e1-e17
International Journal of Molecular Sciences, March 10, 2026, 2547
S0405 AF-353 AF-353 (Ro-4) is a potent, selective and orally bioavailable antagonist of P2X3 receptor and P2X2/3 receptor with pIC50 of 8.06, 8.05 and 7.41 for human P2X3, rat P2X3 and human P2X2/3, respectively.
Cell, 2025, 2687-2704.e29
Cell, 2025, S0092-8674(25)00280-6
Biomedical Chemistry: Research and Methods, 2025, 137-145

Signaling Pathway Map