P2受容体
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) | ||
---|---|---|---|---|
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 |
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 |
S3520 | AZ10606120 dihydrochloride | 17 mg/mL | 99 mg/mL | '''<1 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
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 2578MRS2578 is a potent P2Y6 receptor antagonist with IC50 of 37 nM, exhibits insignificant activity at P2Y1, P2Y2, P2Y4,and P2Y11 receptors. |
||
S1984 |
Ticlopidine HClTiclopidine 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. |
||
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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S3766 |
Tanshinone IIA sulfonate sodiumSodium 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). |
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S4637 |
Prasugrel HydrochloridePrasugrel 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 TetrasodiumCangrelor (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 |
PrasugrelPrasugrel (CS-747, LY640315) is a thienopyridine ADP receptor (P2Y12) antagonist, used for the reduction of thrombotic cardiovascular events. |
||
S4079 |
TicagrelorTicagrelor (AZD 6140, AR-C 126532XX) is the first reversibly binding oral P2Y12 receptor antagonist with Ki of 2 nM. |
![]() ![]() 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).
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E0357新 |
EliapixantEliapixant (BAY1817080) is a highly potent and selective P2X3 receptor antagonist with a mean IC50 of 8 nM. |
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S9498新 |
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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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. |
||
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. |
||
S8519 |
A-317491A-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. |
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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. |
||
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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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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S5057 |
Minodronic acidMinodronic acid (YM529, ONO-5920) is a third-generation nitrogen-cotaining bisphosphonate that is used for the treatment of osteoporosis. |
||
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. |
||
S6592 |
Diquafosol TetrasodiumDiquafosol Tetrasodium (INS-365), a P2Y2 receptor agonist, is a pharmaceutical drug for the treatment of dry eye disease. |
||
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. |
||
S1415 |
Clopidogrel (SR-25990C) BisulfateClopidogrel Bisulfate (SR-25990C, Clopidogrel hydrogen sulfate, Iscover, Plavix) is an oral, thienopyridine class antiplatelet agent. |
![]() ![]() (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. |
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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. |
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 2578MRS2578 is a potent P2Y6 receptor antagonist with IC50 of 37 nM, exhibits insignificant activity at P2Y1, P2Y2, P2Y4,and P2Y11 receptors. |
||
S1984 |
Ticlopidine HClTiclopidine 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. |
||
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. |
||
S3766 |
Tanshinone IIA sulfonate sodiumSodium 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 HydrochloridePrasugrel 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 TetrasodiumCangrelor (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 |
PrasugrelPrasugrel (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 |
TicagrelorTicagrelor (AZD 6140, AR-C 126532XX) is the first reversibly binding oral P2Y12 receptor antagonist with Ki of 2 nM. |
2021, 10.1164/rccm.202009-3686OC 2020, 10 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 |
EliapixantEliapixant (BAY1817080) is a highly potent and selective P2X3 receptor antagonist with a mean IC50 of 8 nM. |
||
S9498新 |
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. |
||
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. |
||
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. |
2022, 10.1002/jcp.30685 2021, 10.1002/1873-3468.14207 2020, 139:75-86 |
|
S8519 |
A-317491A-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 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. |
2021, 9:692028 2021, 14:663649 2021, 12:639558 |
|
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. |
||
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. |
||
S5057 |
Minodronic acidMinodronic acid (YM529, ONO-5920) is a third-generation nitrogen-cotaining bisphosphonate that is used for the treatment of osteoporosis. |
||
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. |
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 TetrasodiumDiquafosol Tetrasodium (INS-365), a P2Y2 receptor agonist, is a pharmaceutical drug for the treatment of dry eye disease. |
||
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. |
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) BisulfateClopidogrel Bisulfate (SR-25990C, Clopidogrel hydrogen sulfate, Iscover, Plavix) is an oral, thienopyridine class antiplatelet agent. |
2021, 10.1111/jth.15593 2020, 33(5):108346 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. |
2021, JVI0148121 2021, 21(1):1307 2020, |
|
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. |