Home Neuronal Signaling P2 Receptor

P2 Receptor Inhibitors

Cat.No. Product Name Information Product Use Citations Product Validations
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
S1984 Ticlopidine HCl Ticlopidine HCl is an P2 receptor inhibitor against ADP-induced platelet aggregation with IC50 of ~2 μM.
J Immunother Cancer, 2024, 12(11)e009805
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.
E7266 Aurintricarboxylic acid Aurintricarboxylic acid is a potent, selective allosteric antagonist of P2X1R and P2X3R, with IC50 of 8.6 nM and 72.9 nM, respectively. It also functions as an anti-influenza agent by inhibiting viral neuraminidase. This compound suppresses apoptosis and is a potent inhibitor of topoisomerase II with an ID50 of ~7 nM in relaxation assays.
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.
S6592 Diquafosol Tetrasodium Diquafosol Tetrasodium (INS-365), a P2Y2 receptor agonist, is a pharmaceutical drug for the treatment of dry eye disease.
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.
S3216 Uridine 5'-diphosphoglucose disodium salt Uridine-5'-diphosphoglucose (UDPG, UDP-Glc, UDP-D-Glucose, UDP-α-D-Glucose) activates the P2Y(14) receptor, a neuroimmune system GPCR. Uridine-5'-diphosphoglucose is the precursor of glucose-containing oligosaccharides, polysaccharides, glycoproteins, and glycolipids in animal tissues and in some microorganisms.
S3368 Uridine-5'-diphosphate disodium salt

Uridine-5'-diphosphate (UDP) disodium salt is a potent, selective and natural agonist of P2Y6 receptor with EC50 = 300 nM and pEC50 of 6.52, respectively. Uridine-5'-diphosphate (UDP) disodium salt is also an antagonist of P2Y14 receptor with pEC50 of 7.28.
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.
S1351 Ivermectin Ivermectin is a glutamate-gated chloride channel (GluCls) activator, used as a broad-spectrum antiparasitic drug. This compound is a specific positive allosteric effector of P2X4 and α7 nicotinic acetylcholine receptors (nAChRs). It is a specific inhibitor of Impα/β1-mediated nuclear import and has potent antiviral activity towards both HIV-1 and dengue virus. This chemical induces autophagy through the AKT/mTOR signaling pathway and mitophagy.
Nat Commun, 2025, 16(1):7156
J Adv Res, 2025, S2090-1232(25)00874-4
Biomed Pharmacother, 2025, 189:118248
S0053 CAY10593 (VU0155069) CAY10593 (VU0155069) is a selective phospholipase D1 (PLD1) antagonist that impairs human P2X7 acivation.
Free Radic Biol Med, 2021, S0891-5849(21)00821-2
S3766 Tanshinone IIA sulfonate sodium Sodium tanshinone IIA sulfonate (STS) is a water-soluble derivative of tanshinone IIA isolated as the main pharmacologically active natural compound from a traditional Chinese herbal medicine, the dried root of Salvia miltiorrhiza Bunge known as Danshen. Sodium tanshinone IIA sulfonate (STS) is a potent negative allosteric modulator of the human purinergic receptor P2X7. Sodium tanshinone IIA sulfonate (STS) inhibits the activity of CYP3A4 and store-operated Ca2+ entry (SOCE) through store-operated Ca2+ channels (SOCC) via downregulating the expression of transient receptor potential canonical proteins (TRPC).
J Inflamm Res, 2022, 15:6293-6306
S3293 Gardenoside Gardenoside is a natural compound extracted from Gardenia fruits, with hepatoprotective properties. It inhibits TNF-α, IL-1β, IL-6 and NFκB activation. This compound also has an inhibitory effect on free fatty acids (FFA)-induced cellular steatosis. It suppresses the pain in rats model of chronic constriction injury by regulating the P2X3 and P2X7 receptors.