P2 Receptor

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P2X receptor P2Y receptor

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P2 Receptor製品

All (33)
P2 Receptor阻害剤 (8)
P2 Receptor拮抗剤(16)
P2 Receptor作動薬(3)
P2 Receptorモジュレータ(3)
新製品

製品コード	製品名称	製品説明	文献中Selleckの製品使用例
S1351	Ivermectin	Ivermectin 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 (MK-933) is a specific inhibitor of Impα/β1-mediated nuclear import and has potent antiviral activity towards both HIV-1 and dengue virus. Ivermectin induces autophagy through the AKT/mTOR signaling pathway and mitophagy.	J Clin Invest, 2024, 134(22)e181314 Viruses, 2024, 16(4)640 Life Sci Alliance, 2023, 6(8)e202302133
S4079	Ticagrelor	Ticagrelor (AZD6140, AR-C 126532XX) is the first reversibly binding oral P2Y12 receptor antagonist with K_i 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
S7705	A-438079 HCl	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
S1415	Clopidogrel (SR-25990C) Bisulfate	Clopidogrel (SR-25990C) Bisulfate is an oral, thienopyridine class antiplatelet agent.	J Immunother Cancer, 2024, 12(11)e009805 Cell Mol Life Sci, 2024, 81(1):116 Int J Mol Sci, 2023, 24(14)11706
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
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.	J Immunother Cancer, 2024, 12(11)e009805 J Thromb Haemost, 2023, S1538-7836(23)00082-X Food Funct, 2021, 10.1039/d1fo00531f
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
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.	Ann Med, 2022, 54(1):1616-1626 Sci Rep, 2021, 11(1):15129
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.	Am J Cancer Res, 2024, 14(2):585-600 Cell Rep, 2023, 42(7):112696
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
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
S3217	Brilliant Blue G	Brilliant Blue G (BBG) is a dye which is commonly used in laboratories to stain or quantify proteins.Brilliant Blue G 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.	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
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.
E1128	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.
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.
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 P2X_2/3 receptors with Ki values of 22 nM and 9 nM for human P2X₃ and P2X_2/3 receptors.
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. 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^New	(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.
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.
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.
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.
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.
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.
S5057	Minodronic acid	Minodronic acid (YM529, ONO-5920) is a third-generation nitrogen-cotaining bisphosphonate that is used for the treatment of osteoporosis.
E1128	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.
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.
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.	J Immunother Cancer, 2024, 12(11)e009805 J Thromb Haemost, 2023, S1538-7836(23)00082-X Food Funct, 2021, 10.1039/d1fo00531f
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.	Ann Med, 2022, 54(1):1616-1626 Sci Rep, 2021, 11(1):15129
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
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
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
E4929^New	(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.
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.
S4079	Ticagrelor	Ticagrelor (AZD6140, AR-C 126532XX) is the first reversibly binding oral P2Y12 receptor antagonist with K_i 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
S7705	A-438079 HCl	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
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
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. 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.	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.Brilliant Blue G 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.	Sci Adv, 2022, 8(18):eabn2879
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. 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.
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 P2X_2/3 receptors with Ki values of 22 nM and 9 nM for human P2X₃ and P2X_2/3 receptors.
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. This product is not soluble in PBS solution. Please do not dissolve it in PBS for administration.
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.
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.
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.
S5057	Minodronic acid	Minodronic acid (YM529, ONO-5920) is a third-generation nitrogen-cotaining bisphosphonate that is used for the treatment of osteoporosis.
E1128	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.
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.
S1351	Ivermectin	Ivermectin 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 (MK-933) is a specific inhibitor of Impα/β1-mediated nuclear import and has potent antiviral activity towards both HIV-1 and dengue virus. Ivermectin induces autophagy through the AKT/mTOR signaling pathway and mitophagy.	J Clin Invest, 2024, 134(22)e181314 Viruses, 2024, 16(4)640 Life Sci Alliance, 2023, 6(8)e202302133
S1415	Clopidogrel (SR-25990C) Bisulfate	Clopidogrel (SR-25990C) Bisulfate is an oral, thienopyridine class antiplatelet agent.	J Immunother Cancer, 2024, 12(11)e009805 Cell Mol Life Sci, 2024, 81(1):116 Int J Mol Sci, 2023, 24(14)11706
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.
E4929^New	(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.

P2 Receptor阻害剤の選択性比較