P2 Receptor
Inhibitory Selectivity
Isoform-specific Inhibitors
P2 Receptor Products
| Catalog No. | Information | Product Use Citations | Product Validations |
|---|---|---|---|
| S2855 |
MRS 2578MRS2578 is a potent P2Y6 receptor antagonist with IC50 of 37 nM, exhibits insignificant activity at P2Y1, P2Y2, P2Y4,and P2Y11 receptors. |
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| S0053 |
CAY10593 (VU0155069)CAY10593 (VU0155069) is a selective phospholipase D1 (PLD1) antagonist that impairs human P2X7 acivation. |
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| S3293 |
GardenosideGardenoside 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. |
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| S0826 |
A-740003A-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. |
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| S0758 |
BX430BX430 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. |
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| E0357New |
EliapixantEliapixant (BAY1817080) is a highly potent and selective P2X3 receptor antagonist with a mean IC50 of 8 nM. |
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| S8725 |
A-804598A-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. |
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| S3520 |
AZ10606120 dihydrochlorideAZ10606120 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. |
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| S7705 |
A-438079 HClA-438079 HCl is a potent, and selective P2X7 receptor antagonist with pIC50 of 6.9. |
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| S6664 |
GefapixantGefapixant (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. |
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| S6087 |
IndophagolinIndophagolin, 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. |
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| S0405 |
AF-353AF-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. |
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| S3217 |
Brilliant Blue GBrilliant 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. |
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| S9498 |
5-BDBD5-BDBD is a potent P2X4R selective antagonist with an IC50 of 0.75 μM when applied for 2 min prior and during ATP stimulation. |
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| E1128New |
BzATP triethylammonium saltBzATP 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. |
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| S3216 |
Uridine 5'-diphosphoglucose disodium saltUridine-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. |
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| S3368 |
Uridine-5'-diphosphate disodium saltUridine-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. |
| Catalog No. | Information | Product Use Citations | Product Validations |
|---|---|---|---|
| S2855 |
MRS 2578MRS2578 is a potent P2Y6 receptor antagonist with IC50 of 37 nM, exhibits insignificant activity at P2Y1, P2Y2, P2Y4,and P2Y11 receptors. |
||
| S0053 |
CAY10593 (VU0155069)CAY10593 (VU0155069) is a selective phospholipase D1 (PLD1) antagonist that impairs human P2X7 acivation. |
||
| S3293 |
GardenosideGardenoside 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. |
| Catalog No. | Information | Product Use Citations | Product Validations |
|---|---|---|---|
| S0826 |
A-740003A-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 |
BX430BX430 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. |
||
| E0357New |
EliapixantEliapixant (BAY1817080) is a highly potent and selective P2X3 receptor antagonist with a mean IC50 of 8 nM. |
||
| S8725 |
A-804598A-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. |
||
| S3520 |
AZ10606120 dihydrochlorideAZ10606120 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. |
||
| S7705 |
A-438079 HClA-438079 HCl is a potent, and selective P2X7 receptor antagonist with pIC50 of 6.9. |
||
| S6664 |
GefapixantGefapixant (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 |
IndophagolinIndophagolin, 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-353AF-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. |
||
| S3217 |
Brilliant Blue GBrilliant 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. |
||
| S9498 |
5-BDBD5-BDBD is a potent P2X4R selective antagonist with an IC50 of 0.75 μM when applied for 2 min prior and during ATP stimulation. |
| Catalog No. | Information | Product Use Citations | Product Validations |
|---|---|---|---|
| E1128New |
BzATP triethylammonium saltBzATP 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 saltUridine-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. |
| Catalog No. | Information | Product Use Citations | Product Validations |
|---|---|---|---|
| S3368 |
Uridine-5'-diphosphate disodium saltUridine-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. |
