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)
DMSO アルコール
S2855 MRS 2578 <1 mg/mL 42 mg/mL <1 mg/mL
S3293 Gardenoside -1 mg/mL 81 mg/mL -1 mg/mL
S1984 Ticlopidine HCl 4 mg/mL 1 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
S3520 AZ10606120 dihydrochloride 17 mg/mL 99 mg/mL '''<1 mg/mL
S0053 CAY10593 (VU0155069) <1 mg/mL 30 mg/mL <1 mg/mL
S3217 Brilliant Blue G 100 mg/mL 100 mg/mL 4 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
S3216 Uridine 5'-diphosphoglucose disodium salt 100 mg/mL 100 mg/mL <1 mg/mL
S6592 Diquafosol Tetrasodium 100 mg/mL 50 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

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.

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.

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, AR-C 126532XX) is the first reversibly binding oral P2Y12 receptor antagonist with Ki of 2 nM.

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.

S0053

CAY10593 (VU0155069)

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

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.

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.

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.

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.

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.

S1415

Clopidogrel (SR-25990C) Bisulfate

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

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.

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
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.

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.

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.

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.

2018, 15(5):6107-6114

2017, 42(6):755-761

S4079

Ticagrelor

Ticagrelor (AZD 6140, AR-C 126532XX) is the first reversibly binding oral P2Y12 receptor antagonist with Ki of 2 nM.

2020, 10

2020, 12(1)

2018, 10.1111/jth.14318

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.

S0053

CAY10593 (VU0155069)

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

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.

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.

2020, 139:75-86

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.

2021, 14:663649

2021, 12:639558

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.

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
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.

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.

2020, 33(5):108346

2020, ATVBAHA120314571

2019, 16(1):217

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.

2020,

2020, 10(6):72

2020, 12(9)E2668

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.