P2 Receptor

Signaling Pathway Map

Research Area

Inhibitory Selectivity

Isoform-specific Inhibitors

P2 Receptor Products

Catalog No. Information Product Use Citations Product Validations
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.

S3293New

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.

S1984

Ticlopidine HCl

Ticlopidine HCl is an P2 receptor inhibitor against ADP-induced platelet aggregation with IC50 of ~2 μM.

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 (LY 640315) is a piperazine derivative and pletelet aggregation inhibitor that is used to prevent thrombosis in patients with acute coronary syndrome.

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.

S1258

Prasugrel

Prasugrel (CS-747, LY640315) is a thienopyridine ADP receptor (P2Y12) antagonist, used for the reduction of thrombotic cardiovascular events.

S4079

Ticagrelor

Ticagrelor (AZD 6140) is the first reversibly binding oral P2Y12 receptor antagonist with Ki of 2 nM.

S0053New

CAY10593 (VU0155069)

CAY10593 (VU0155069) is a selective phospholipase D1 (PLD1) antagonist that impairs human P2X7 acivation.

S3217New

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.

S0758New

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.

S0405New

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.

S6664New

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.

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.

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.

S7705

A-438079 HCl

A-438079 HCl is a potent, and selective P2X7 receptor antagonist with pIC50 of 6.9.

S5057

Minodronic acid

Minodronic acid (YM529) 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.

S3216New

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.

S1415

Clopidogrel Bisulfate

Clopidogrel Bisulfate (SR-25990C) is an oral, thienopyridine class antiplatelet agent.

S1351

Ivermectin

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.

Catalog No. Information Product Use Citations Product Validations
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.

S3293New

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.

S1984

Ticlopidine HCl

Ticlopidine HCl is an P2 receptor inhibitor against ADP-induced platelet aggregation with IC50 of ~2 μM.

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 (LY 640315) is a piperazine derivative and pletelet aggregation inhibitor that is used to prevent thrombosis in patients with acute coronary syndrome.

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.

Catalog No. Information Product Use Citations Product Validations
S1258

Prasugrel

Prasugrel (CS-747, LY640315) is a thienopyridine ADP receptor (P2Y12) antagonist, used for the reduction of thrombotic cardiovascular events.

S4079

Ticagrelor

Ticagrelor (AZD 6140) is the first reversibly binding oral P2Y12 receptor antagonist with Ki of 2 nM.

S0053New

CAY10593 (VU0155069)

CAY10593 (VU0155069) is a selective phospholipase D1 (PLD1) antagonist that impairs human P2X7 acivation.

S3217New

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.

S0758New

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.

S0405New

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.

S6664New

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.

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.

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.

S7705

A-438079 HCl

A-438079 HCl is a potent, and selective P2X7 receptor antagonist with pIC50 of 6.9.

S5057

Minodronic acid

Minodronic acid (YM529) 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.

Catalog No. Information Product Use Citations Product Validations
S3216New

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.

Catalog No. Information Product Use Citations Product Validations
S1415

Clopidogrel Bisulfate

Clopidogrel Bisulfate (SR-25990C) is an oral, thienopyridine class antiplatelet agent.

S1351

Ivermectin

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.