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P2 Receptor Antagonists

Cat.No. Product Name Information Product Use Citations Product Validations
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
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
Evid Based Complement Alternat Med, 2022, 2022:7941039
Am J Respir Crit Care Med, 2021, 10.1164/rccm.202009-3686OC
Verified customer review of Ticagrelor
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
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.
Oncol Lett, 2018, 15(5):6107-6114
J Toxicol Sci, 2017, 42(6):755-761
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.
Am J Cancer Res, 2024, 14(2):585-600
Cell Rep, 2023, 42(7):112696
S3217 Brilliant Blue G Brilliant Blue G (BBG) is a dye which is commonly used in laboratories to stain or quantify proteins. This compound is a potent non-competitive antagonist of P2X7 receptor with IC50 of 10.1 nM and 265 nM for rat P2X7 and human P2X7, respectively.
Am J Cancer Res, 2024, 14(2):585-600
J Immunol, 2023, 210(12):1962-73
S9498 5-BDBD

5-BDBD is a potent P2X4R selective antagonist with an IC50 of 0.75 μM when applied for 2 min prior and during ATP stimulation.
Biol Pharm Bull, 2025, 48(5):657-671
Sci Adv, 2022, 8(18):eabn2879
S6664 Gefapixant Gefapixant (AF-219, MK-7264, R1646, RG-1646, RO 4926219) is an orally active small molecule antagonist of human P2X3 receptor with IC50 of about 30 nM, 100–250 nM for recombinant hP2X3 homotrimers and hP2X2/3 heterotrimeric receptors, respectively. This compound has shown promise for the treatment of refractory and unexplained chronic cough.
bioRxiv, 2025, 2025.05.01.651726
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, S0092-8674(25)00280-6
S8513 JNJ-47965567 JNJ-47965567 is a centrally permeable, high-affinity, selective P2X7 antagonist, which can be used to probe the role of central P2X7 in rodent models of CNS pathophysiology.
S0758 BX430 BX430 is a potent and selective noncompetitive allosteric antagonist of human P2X4 receptor channels with IC50 of 0.54 μM. This compound is a potent antagonist of zebrafish P2X4 but has no effect on rat and mouse P2X4 orthologs. It is used for chronic pain and cardiovascular disease.
E0357 Eliapixant

Eliapixant (BAY1817080) is a highly potent and selective P2X3 receptor antagonist with a mean IC50 of 8 nM.
S8519 A-317491 A-317491 is a novel potent and selective non-nucleotide antagonist of P2X3 and P2X2/3 receptors with Ki values of 22 nM and 9 nM for human P2X3 and P2X2/3 receptors.
S3520 AZ10606120 dihydrochloride AZ10606120 dihydrochloride (2HCl) is a potent and selective antagonist for P2X7 receptor (P2X7R) with IC50 of ~10 nM. This compound exhibits anti-depressant effects and reduces tumour growth. This product is not soluble in PBS solution. Please do not dissolve it in PBS for administration.
S6087 Indophagolin Indophagolin, a potent indoline-containing autophagy inhibitor with IC50 of 140 nM, antagonizes the purinergic receptor P2X4 as well as P2X1 and P2X3 with IC50s of 2.71, 2.40 and 3.49 μM, respectively, also has a strong antagonistic effect on serotonin receptor 5-HT6 with IC50 of 1.0 μM.
S5057 Minodronic acid Minodronic acid (YM529, ONO-5920) is a third-generation nitrogen-cotaining bisphosphonate that is used for the treatment of osteoporosis. This compound is an aminobisphosphonate that is a selective antagonist of purinergic P2X2/3 receptors involved in pain.