P2受容体

シグナル伝達経路

研究分野

阻害剤の選択性比較

カタログ番号	製品カタログ	溶解度(25°C)
カタログ番号	製品カタログ	水	DMSO	アルコール
S2855	MRS 2578	<1 mg/mL	42 mg/mL	<1 mg/mL
S1984	Ticlopidine HCl	4 mg/mL	1 mg/mL	1 mg/mL
S0053	CAY10593 (VU0155069)	<1 mg/mL	30 mg/mL	<1 mg/mL
S3293	Gardenoside	-1 mg/mL	81 mg/mL	-1 mg/mL
S3766	Tanshinone IIA sulfonate sodium	-1 mg/mL	79 mg/mL	-1 mg/mL
S4637	Prasugrel Hydrochloride	<1 mg/mL	46 mg/mL	9 mg/mL
S3737	Cangrelor Tetrasodium	100 mg/mL	2 mg/mL	<1 mg/mL
S1258	Prasugrel	<1 mg/mL	30 mg/mL	7 mg/mL
S4079	Ticagrelor	<1 mg/mL	100 mg/mL	'53 mg/mL
E0357	Eliapixant	<1 mg/mL	96 mg/mL	5 mg/mL
S9498	5-BDBD	<1 mg/mL	71 mg/mL	'<1 mg/mL
S3520	AZ10606120 dihydrochloride	17 mg/mL	99 mg/mL	'''<1 mg/mL
S0826	A-740003	<1 mg/mL	95 mg/mL	'''1.5 mg/mL
S0758	BX430	<1 mg/mL	83 mg/mL	83 mg/mL
S8725	A-804598	<1 mg/mL	63 mg/mL	6 mg/mL
S8519	A-317491	<1 mg/mL	100 mg/mL	100 mg/mL
S7705	A-438079 HCl	61 mg/mL	61 mg/mL	20 mg/mL
S6664	Gefapixant	<1 mg/mL	71 mg/mL	<1 mg/mL
S0405	AF-353	<1 mg/mL	100 mg/mL	4 mg/mL
S5057	Minodronic acid	<1 mg/mL	0.001 mg/mL	'<1 mg/mL
S3217	Brilliant Blue G	100 mg/mL	100 mg/mL	4 mg/mL
S6592	Diquafosol Tetrasodium	100 mg/mL	50 mg/mL	<1 mg/mL
S3216	Uridine 5'-diphosphoglucose disodium salt	100 mg/mL	100 mg/mL	<1 mg/mL
S1415	Clopidogrel (SR-25990C) Bisulfate	78 mg/mL	83 mg/mL	'''46 mg/mL
S1351	Ivermectin (MK-933)	<1 mg/mL	100 mg/mL	''28 mg/mL
S3368	Uridine-5'-diphosphate disodium salt	90 mg/mL	<1 mg/mL	'''<1 mg/mL

亜型選択性的な製品

P2 Receptor製品

All (26) P2 Receptor阻害剤(7) P2 Receptor拮抗剤(14) P2 Receptor作動薬(2) P2 Receptorモジュレータ(3)

製品コード	製品説明	文献中Selleckの製品使用例	お客様のフィードバック
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
S1984	Ticlopidine HCl Ticlopidine HCl is an P2 receptor inhibitor against ADP-induced platelet aggregation with IC50 of ~2 μM.
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. 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.
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.	Oncol Lett, 2018, 15(5):6107-6114
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
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
S4079	Ticagrelor Ticagrelor (AZD 6140, AR-C 126532XX) is the first reversibly binding oral P2Y12 receptor antagonist with K_i 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)	Effect of antiplatelet drugs on platelet aggregation in healthy individuals. Samples from healthy individuals were preincubated with anti-platelet drugs (n = 3). Curves and columns show mean platelet aggregation and the relationship between platelet aggregation and drug concen-tration. Bars represent standard deviations. *P < 0.05 as compared with platelet aggregation with the same agonist but no drugs added; pairedStudent’s t-test. (A-C) The drugs tested were abciximab (A), ticagrelor (B), and vorapaxar (C).
E0357^新	Eliapixant Eliapixant (BAY1817080) is a highly potent and selective P2X3 receptor antagonist with a mean IC50 of 8 nM.
S9498^新	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.
S3520^新	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.
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.
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.
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.	FEBS Lett, 2021, 10.1002/1873-3468.14207 J Mol Cell Cardiol, 2020, 139:75-86
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.
S7705	A-438079 HCl A-438079 HCl is a potent, and selective P2X7 receptor antagonist with pIC50 of 6.9.	Front Mol Neurosci, 2021, 14:663649 Front Pharmacol, 2021, 12:639558 Life Sci, 2021, S0024-3205(21)00216-2
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.
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.
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.
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.
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	(A) HPLC glycan traces of IgG recovered from joint after K/BxN and PBS or B4ST6Fc treatment with or without clopidogrel. (B) Ratios of monosialylated and agalactosylated glycans (S1/G0) from IgG described in (A).
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,
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.

製品コード	製品説明	文献中Selleckの製品使用例
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
S1984	Ticlopidine HCl Ticlopidine HCl is an P2 receptor inhibitor against ADP-induced platelet aggregation with IC50 of ~2 μM.
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. 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.
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.	Oncol Lett, 2018, 15(5):6107-6114
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

製品コード	製品説明	文献中Selleckの製品使用例	お客様のフィードバック
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
S4079	Ticagrelor Ticagrelor (AZD 6140, AR-C 126532XX) is the first reversibly binding oral P2Y12 receptor antagonist with K_i 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)	Effect of antiplatelet drugs on platelet aggregation in healthy individuals. Samples from healthy individuals were preincubated with anti-platelet drugs (n = 3). Curves and columns show mean platelet aggregation and the relationship between platelet aggregation and drug concen-tration. Bars represent standard deviations. *P < 0.05 as compared with platelet aggregation with the same agonist but no drugs added; pairedStudent’s t-test. (A-C) The drugs tested were abciximab (A), ticagrelor (B), and vorapaxar (C).
E0357^新	Eliapixant Eliapixant (BAY1817080) is a highly potent and selective P2X3 receptor antagonist with a mean IC50 of 8 nM.
S9498^新	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.
S3520^新	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.
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.
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.
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.	FEBS Lett, 2021, 10.1002/1873-3468.14207 J Mol Cell Cardiol, 2020, 139:75-86
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.
S7705	A-438079 HCl A-438079 HCl is a potent, and selective P2X7 receptor antagonist with pIC50 of 6.9.	Front Mol Neurosci, 2021, 14:663649 Front Pharmacol, 2021, 12:639558 Life Sci, 2021, S0024-3205(21)00216-2
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.
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.
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.

製品コード	製品説明	文献中Selleckの製品使用例	お客様のフィードバック
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.

製品コード

製品説明

文献中Selleckの製品使用例

お客様のフィードバック

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.

製品コード	製品説明	文献中Selleckの製品使用例	お客様のフィードバック
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	(A) HPLC glycan traces of IgG recovered from joint after K/BxN and PBS or B4ST6Fc treatment with or without clopidogrel. (B) Ratios of monosialylated and agalactosylated glycans (S1/G0) from IgG described in (A).
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,
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.

製品コード

製品説明

文献中Selleckの製品使用例

お客様のフィードバック

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

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,

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.