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. |
-
Life Sci Alliance, 2023, 6(8)e202302133
-
Cell Rep Methods, 2023, 3(10):100599
-
Front Pharmacol, 2022, 13:934746
|
|
S4079 |
Ticagrelor
|
Ticagrelor (AZD6140, AR-C 126532XX) is the first reversibly binding oral P2Y12 receptor antagonist with Ki of 2 nM. |
-
Evid Based Complement Alternat Med, 2022, 2022:7941039
-
Am J Respir Crit Care Med, 2021, 10.1164/rccm.202009-3686OC
-
Cell Mol Immunol, 2020, 10
|
|
S7705 |
A-438079 HCl
|
A-438079 HCl is a potent, and selective P2X7 receptor antagonist with pIC50 of 6.9.
|
-
Cells, 2023, 12(23)2696
-
Biomol Biomed, 2023, 23(5):825-837
-
Life Sci, 2021, S0024-3205(21)00216-2
|
|
S1415 |
Clopidogrel (SR-25990C) Bisulfate
|
Clopidogrel (SR-25990C) Bisulfate is an oral, thienopyridine class antiplatelet agent. |
-
Int J Mol Sci, 2023, 24(14)11706
-
Mol Ther, 2022, S1525-0016(22)00420-8
-
J Thromb Haemost, 2021, 10.1111/jth.15593
|
|
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 Thromb Haemost, 2023, S1538-7836(23)00082-X
-
Food Funct, 2021, 10.1039/d1fo00531f
-
Sci Rep, 2018, 8(1):9987
|
|
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. |
-
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. |
|
|
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 P2X2/3 receptors with Ki values of 22 nM and 9 nM for human P2X3 and P2X2/3 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. |
|
|
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. Minodronic acid is an aminobisphosphonate that is a selective antagonist of purinergic P2X2/3 receptors involved in pain. |
|
|
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 Thromb Haemost, 2023, S1538-7836(23)00082-X
- Food Funct, 2021, 10.1039/d1fo00531f
- Sci Rep, 2018, 8(1):9987
|
|
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. |
- 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. |
|
|
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 Ki of 2 nM. |
- Evid Based Complement Alternat Med, 2022, 2022:7941039
- Am J Respir Crit Care Med, 2021, 10.1164/rccm.202009-3686OC
- Cell Mol Immunol, 2020, 10
|
|
S7705 |
A-438079 HCl
|
A-438079 HCl is a potent, and selective P2X7 receptor antagonist with pIC50 of 6.9.
|
- Cells, 2023, 12(23)2696
- Biomol Biomed, 2023, 23(5):825-837
- Life Sci, 2021, S0024-3205(21)00216-2
|
|
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 P2X2/3 receptors with Ki values of 22 nM and 9 nM for human P2X3 and P2X2/3 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. Minodronic acid is an aminobisphosphonate that is a selective antagonist of purinergic P2X2/3 receptors involved in pain. |
|
|