Home Neuronal Signaling P2 Receptor

P2 Receptor Inhibitors

Cat.No. Product Name Information Product Use Citations Product Validations
S1984 Ticlopidine HCl Ticlopidine HCl is an P2 receptor inhibitor against ADP-induced platelet aggregation with IC50 of ~2 μM.
Nature, 2025, 423-431
J Immunother Cancer, 2024, 12(11)e009805
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
S4637 Prasugrel Hydrochloride Prasugrel hydrochloride (Prasugrel HCl, LY640315,PCR 4099 Hydrochloride) is a piperazine derivative and pletelet aggregation inhibitor that is used to prevent thrombosis in patients with acute coronary syndrome.
J Immunother Cancer, 2024, 12(11)e009805
Oncol Lett, 2018, 15(5):6107-6114
Oncology Letters, 2018, 6107-6114
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
Science Advances, 2022, eabn2879
Sci Adv, 2022, 8(18):eabn2879
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.
Biochemical Journal, August 14, 2018, 2417-2433
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.
Journal of Pharmacological Sciences, 2022, 255-261
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
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.
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.
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.
E1593New Camlipixant Camlipixant (BLU-5937) is a potent, selective, non-competitive antagonist that target P2X3 homotrimeric receptor, with an IC50 of 25 nM for hP2X3 homotrimeric form.
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
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).
Journal of Inflammation Research, 2022, 6293-6306
J Inflamm Res, 2022, 15:6293-6306
Molecular Medicine Reports, 2017, 1612-1618
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
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.
Current Issues in Molecular Biology, 2022, 1046-1061