P2 Receptor

Choose Selective P2 Receptor Inhibitors

P2 Receptor Signaling Pathway Map

P2 Receptor Signaling Pathways

P2 Receptor Products

  • All (28)
  • P2 Receptor Inhibitors (7)
  • P2 Receptor Antagonists (15)
  • P2 Receptor Agonists (3)
  • P2 Receptor Modulators (3)
  • New P2 Receptor Products
Catalog No. Product Name Information Product Use Citations Product Validations
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
S1984 Ticlopidine HCl Ticlopidine HCl is an P2 receptor inhibitor against ADP-induced platelet aggregation with IC50 of ~2 μM.
S2855 MRS 2578 MRS2578 is a potent P2Y6 receptor antagonist with IC50 of 37 nM, exhibits insignificant activity at P2Y1, P2Y2, P2Y4,and P2Y11 receptors.
Sci Rep, 2021, 11(1):15129
S3293 Gardenoside Gardenoside is a natural compound extracted from Gardenia fruits, with hepatoprotective properties. Gardenoside inhibits TNF-α, IL-1β, IL-6 and NFκB activation. Gardenoside also has an inhibitory effect on free fatty acids (FFA)-induced cellular steatosis. Gardenoside suppresses the pain in rats model of chronic constriction injury by regulating the P2X3 and P2X7 receptors.
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.
Food Funct, 2021, 10.1039/d1fo00531f
Sci Rep, 2018, 8(1):9987
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).
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.
Oncol Lett, 2018, 15(5):6107-6114
E0357New Eliapixant

Eliapixant (BAY1817080) is a highly potent and selective P2X3 receptor antagonist with a mean IC50 of 8 nM.

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.
S0758 BX430 BX430 is a potent and selective noncompetitive allosteric antagonist of human P2X4 receptor channels with IC50 of 0.54 μM. BX430 is a potent antagonist of zebrafish P2X4 but has no effect on rat and mouse P2X4 orthologs. BX430 is used for chronic pain and cardiovascular disease.
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. A-740003 potently blocks agonist-evoked IL-1β release and pore formation with IC50 of 156 nM and 92 nM in differentiated human THP-1 cells.
S1258 Prasugrel Prasugrel (CS-747, LY640315) 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
S3217 Brilliant Blue G Brilliant Blue G (BBG) 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. Brilliant Blue G is a dye which is commonly used in laboratories to stain or quantify proteins.
S3520 AZ10606120 dihydrochloride AZ10606120 dihydrochloride (2HCl) is a potent and selective antagonist for P2X7 receptor (P2X7R) with IC50 of ~10 nM. AZ10606120 dihydrochloride exhibits anti-depressant effects and reduces tumour growth.
S4079 Ticagrelor Ticagrelor (AZD 6140, AR-C 126532XX) is the first reversibly binding oral P2Y12 receptor antagonist with Ki of 2 nM.
Am J Respir Crit Care Med, 2021, 10.1164/rccm.202009-3686OC
Cell Mol Immunol, 2020, 10
Cancers (Basel), 2020, 12(1)
S5057 Minodronic acid Minodronic acid (YM529, ONO-5920) is a third-generation nitrogen-cotaining bisphosphonate that is used for the treatment of osteoporosis. Minodronic acid is an aminobisphosphonate that is a selective antagonist of purinergic P2X2/3 receptors involved in pain.
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.
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. Gefapixant has shown promise for the treatment of refractory and unexplained chronic cough.
S7705 A-438079 HCl A-438079 HCl is a potent, and selective P2X7 receptor antagonist with pIC50 of 6.9.
Front Cell Dev Biol, 2021, 9:692028
Front Mol Neurosci, 2021, 14:663649
Front Pharmacol, 2021, 12:639558
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.
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.
J Cell Physiol, 2022, 10.1002/jcp.30685
FEBS Lett, 2021, 10.1002/1873-3468.14207
J Mol Cell Cardiol, 2020, 139:75-86
S9498New 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.

Sci Adv, 2022, 8(18):eabn2879
E1128New 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.
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.
S6592 Diquafosol Tetrasodium Diquafosol Tetrasodium (INS-365), a P2Y2 receptor agonist, is a pharmaceutical drug for the treatment of dry eye disease.
S1351 Ivermectin (MK-933) Ivermectin (MK-933, IVM) is a glutamate-gated chloride channel (GluCls) activator, used as a broad-spectrum antiparasitic drug. Ivermectin (MK-933, IVM) is a specific positive allosteric effector of P2X4 and α7 nicotinic acetylcholine receptors (nAChRs). Ivermectin has potent antiviral activity towards both HIV-1 and dengue virus. Ivermectin induces autophagy through the AKT/mTOR signaling pathway and mitophagy.
J Virol, 2021, JVI0148121
BMC Cancer, 2021, 21(1):1307
Nat Cell Biol, 2020,
S1415 Clopidogrel (SR-25990C) Bisulfate Clopidogrel Bisulfate (SR-25990C, Clopidogrel hydrogen sulfate, Iscover, Plavix) is an oral, thienopyridine class antiplatelet agent.
J Thromb Haemost, 2021, 10.1111/jth.15593
Cell Rep, 2020, 33(5):108346
Arterioscler Thromb Vasc Biol, 2020, ATVBAHA120314571
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.

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
S1984 Ticlopidine HCl Ticlopidine HCl is an P2 receptor inhibitor against ADP-induced platelet aggregation with IC50 of ~2 μM.
S2855 MRS 2578 MRS2578 is a potent P2Y6 receptor antagonist with IC50 of 37 nM, exhibits insignificant activity at P2Y1, P2Y2, P2Y4,and P2Y11 receptors.
Sci Rep, 2021, 11(1):15129
S3293 Gardenoside Gardenoside is a natural compound extracted from Gardenia fruits, with hepatoprotective properties. Gardenoside inhibits TNF-α, IL-1β, IL-6 and NFκB activation. Gardenoside also has an inhibitory effect on free fatty acids (FFA)-induced cellular steatosis. Gardenoside suppresses the pain in rats model of chronic constriction injury by regulating the P2X3 and P2X7 receptors.
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.
Food Funct, 2021, 10.1039/d1fo00531f
Sci Rep, 2018, 8(1):9987
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).
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.
Oncol Lett, 2018, 15(5):6107-6114
E0357New Eliapixant

Eliapixant (BAY1817080) is a highly potent and selective P2X3 receptor antagonist with a mean IC50 of 8 nM.

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.
S0758 BX430 BX430 is a potent and selective noncompetitive allosteric antagonist of human P2X4 receptor channels with IC50 of 0.54 μM. BX430 is a potent antagonist of zebrafish P2X4 but has no effect on rat and mouse P2X4 orthologs. BX430 is used for chronic pain and cardiovascular disease.
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. A-740003 potently blocks agonist-evoked IL-1β release and pore formation with IC50 of 156 nM and 92 nM in differentiated human THP-1 cells.
S1258 Prasugrel Prasugrel (CS-747, LY640315) 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
S3217 Brilliant Blue G Brilliant Blue G (BBG) 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. Brilliant Blue G is a dye which is commonly used in laboratories to stain or quantify proteins.
S3520 AZ10606120 dihydrochloride AZ10606120 dihydrochloride (2HCl) is a potent and selective antagonist for P2X7 receptor (P2X7R) with IC50 of ~10 nM. AZ10606120 dihydrochloride exhibits anti-depressant effects and reduces tumour growth.
S4079 Ticagrelor Ticagrelor (AZD 6140, AR-C 126532XX) is the first reversibly binding oral P2Y12 receptor antagonist with Ki of 2 nM.
Am J Respir Crit Care Med, 2021, 10.1164/rccm.202009-3686OC
Cell Mol Immunol, 2020, 10
Cancers (Basel), 2020, 12(1)
S5057 Minodronic acid Minodronic acid (YM529, ONO-5920) is a third-generation nitrogen-cotaining bisphosphonate that is used for the treatment of osteoporosis. Minodronic acid is an aminobisphosphonate that is a selective antagonist of purinergic P2X2/3 receptors involved in pain.
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.
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. Gefapixant has shown promise for the treatment of refractory and unexplained chronic cough.
S7705 A-438079 HCl A-438079 HCl is a potent, and selective P2X7 receptor antagonist with pIC50 of 6.9.
Front Cell Dev Biol, 2021, 9:692028
Front Mol Neurosci, 2021, 14:663649
Front Pharmacol, 2021, 12:639558
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.
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.
J Cell Physiol, 2022, 10.1002/jcp.30685
FEBS Lett, 2021, 10.1002/1873-3468.14207
J Mol Cell Cardiol, 2020, 139:75-86
S9498New 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.

Sci Adv, 2022, 8(18):eabn2879
E1128New 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.
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.
S6592 Diquafosol Tetrasodium Diquafosol Tetrasodium (INS-365), a P2Y2 receptor agonist, is a pharmaceutical drug for the treatment of dry eye disease.
S1351 Ivermectin (MK-933) Ivermectin (MK-933, IVM) is a glutamate-gated chloride channel (GluCls) activator, used as a broad-spectrum antiparasitic drug. Ivermectin (MK-933, IVM) is a specific positive allosteric effector of P2X4 and α7 nicotinic acetylcholine receptors (nAChRs). Ivermectin has potent antiviral activity towards both HIV-1 and dengue virus. Ivermectin induces autophagy through the AKT/mTOR signaling pathway and mitophagy.
J Virol, 2021, JVI0148121
BMC Cancer, 2021, 21(1):1307
Nat Cell Biol, 2020,
S1415 Clopidogrel (SR-25990C) Bisulfate Clopidogrel Bisulfate (SR-25990C, Clopidogrel hydrogen sulfate, Iscover, Plavix) is an oral, thienopyridine class antiplatelet agent.
J Thromb Haemost, 2021, 10.1111/jth.15593
Cell Rep, 2020, 33(5):108346
Arterioscler Thromb Vasc Biol, 2020, ATVBAHA120314571
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.

E0357New Eliapixant

Eliapixant (BAY1817080) is a highly potent and selective P2X3 receptor antagonist with a mean IC50 of 8 nM.

S9498New 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.

Sci Adv, 2022, 8(18):eabn2879
E1128New 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.
Tags: P2 Receptor inhibitor|P2 Receptor agonist|P2 Receptor activator|P2 Receptor inducer|P2 Receptor antagonist|P2 Receptor signaling pathway|P2 Receptor assay kit