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Membrane transporter/Ion channel

Monoamine Transporter

(18)

Monocarboxylate transporter

Na-K-Cl cotransporter

Sodium-dependent phosphate transporter

Neuroscience

Melanocortin Receptor

Neuropeptide Y Receptor

Serotonin Transporter

(54)

iGluR

(143)

P2X Receptor

The ATP-gated P2X receptor cation channel family, or simply P2X receptor family, consists of cation-permeable ligand-gated ion channels that open in response to the binding of extracellular adenosine 5'-triphosphate (ATP). They belong to a larger family of receptors known as the ENaC/P2X superfamily. ENaC and P2X receptors have similar 3-D structures and are homologous. P2X receptors are present in a diverse array of organisms including humans, mouse, rat, rabbit, chicken, zebrafish, bullfrog, fluke, and amoeba.

Filter HomeSignaling PathwaysNeuroscience-Membrane transporter/Ion channelP2X Receptor

JNJ-55308942

T378062166558-11-6In house

JNJ-55308942 is a selective and brain-penetrant antagonist of P2X7 functional with IC50s of 10 and 15 nM and Kis of 7.1 and 2.9 nM for hP2X7 and rP2X7, respectively.

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BzATP triethylammonium salt

TP2226112898-15-4

BzATP triethylammonium salt is a P2X7 receptor agonist.

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JNJ-54175446

T156221627902-21-9In house

JNJ-54175446 (JNJ-5446) is a CNS-permeable and selective P2X7 receptor antagonist that attenuates the release of IL-1β IL-18 from microglia, and may be used in the study of depression.

$293

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Camlipixant

T678851621164-74-6

Camlipixant (BLU-5937) is an orally active purine P2X3 receptor antagonist that is potent, selective and competitive. camlipixant has an IC50 of 25 nM for the hP2X3 homotrimer. camlipixant can be used for the treatment of respiratory disorders and Camlipixant has a strong cough suppressant effect.

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5-BDBD

T22518768404-03-1

5-BDBD is a potent and selective P2X4 receptor antagonist. 5-BDBD inhibits rP2X4R-mediated currents with an IC50 of 0.75 μM. 5-BDBD completely blocked the basal and acute hyperalgesia induced by NTG.

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A 438079

T10207899507-36-9

A 438079 is a potent and selective antagonist of the P2X7 receptor (pIC50: 6.9).

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α,β-Methylene ATP trisodium

T135411343364-54-4

α,β-Methylene ATP trisodium, a phosphonate analog of ATP, is a selective P2X agonist that induces enhanced contraction of UBSM. α,β-Methylene ATP trisodium inhibits P2X1 and P2X3, but is inactive against P2X2, 4 and 7.

$1,650

8-10 weeks

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NP-1815-PX

T711551239578-80-3

NP-1815-PX is a selective P2X4 receptor antagonist with anti-inflammatory and analgesic properties. It inhibits guinea pig tracheal bronchial smooth muscle contraction and can be used to study chronic pain.

$293

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PSB-12062

T1256855476-47-6

PSB-12062 (N-(p-Methylphenylsulfonyl)phenoxazine) is a potent and selective antagonist of P2X4(IC50 of 1.38 μM for human P2X4).

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Ivermectin

T113170288-86-7

Ivermectin (MK-933) is an activator of glutamate-gated chloride channels (GluCls) with antiparasitic activity.

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CE-224535

T14920724424-43-5

CE-224535 (PF-04905428) is a selective antagonist of P2X7 receptor. CE-224535 can be used in disease-modifying antirheumatic studies.

$118

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ATP disodium salt

T1352987-65-5

ATP disodium salt (Adenosine-Triphosphate) is a P2 purinoceptor agonist.

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Opiranserin hydrochloride

T98331440796-75-7

Opiranserin (VVZ-149) hydrochloride is a dual antagonist of glycine transporter type 2 (GlyT2) and serotonin receptor 2A (5HT2A), with IC50s of 0.86 and 1.3 μM, respectively. It shows antagonistic activity on rP2X3 (IC50=0.87 μM). It is development as an injectable agent for the treatment of postoperative pain.

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A-804598

T36391125758-85-1

A-804598 is a competitive and selective P2X7 receptor antagonist (IC50: 10 nM, rat; 9 nM, mouse; 11 nM, human).

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Eliapixant

T95191948229-21-7

Eliapixant (BAY 1817080) (BAY 1817080) is a potent and selective P2X3 receptor antagonist, with an IC50 of 8 nM. Eliapixant can be used for the research of refractory chronic cough.

$135

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Gefapixant

T50991015787-98-0

Gefapixant (AF219) is a P2X3 receptor (P2X3R) antagonist with IC50 of ~30 nM at recombinant hP2X3 homotrimers and 100-250 nM at hP2X2 3 heterotrimeric receptors.

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Lu AF27139

T97862097117-06-9

Lu AF27139 is an effective and selective antagonist of P2X7 receptor (IC50s of 12 and 2.4 nM for human and rat, Kis of 22, 54, and 13 nM for mouse, human, and rat, respectively). Lu AF27139 can be used in CNS diseases studies.

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Aurintricarboxylic acid

T83334431-00-9

Aurintricarboxylic acid (NSC-4056) is a strong inhibitor of topoisomerases and other nucleases. It is a potent inhibitor of ribonuclease and topoisomerase II by preventing the binding of the nucleic acid to the enzyme.

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A 438079 hydrochloride

T2673899431-18-6

A 438079 hydrochloride (A-438079 HCl) is a potent and selective P2X7 receptor antagonist with pIC50 of 6.9.

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GSK-1482160

T610251001389-72-5

GSK-1482160 is a CNS-penetrant negative allosteric modulator of P2X7 receptor with oral activity. The P2X7 receptor is involved in the production of pro-inflammatory cytokines by central and peripheral immune cells, so GSK-1482160 has the potential to study inflammatory diseases. GSK-1482160 shows excellent in vitro potency (in functional and electrophysiological assays at recombinant and naive P2X7 receptors across multiple species including humans) and cross-target selectivity.

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RO-3

T55131026582-88-6

RO3 is a selective antagonist of homomeric P2X3 and heteromeric P2X2 3 receptor

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KN-62

T2694127191-97-3

KN-62 is a potent and specific Ca2+ calmodulin-dependent protein kinase II (CaMKII) inhibitor with Ki of 0.9 μM.

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PPADS tetrasodium

T16564192575-19-2

PPADS tetrasodiuma is a potent P2X receptor antagonist and inhibitor of the inverse mode of Na Ca²⁺ exchange in guinea pig airway smooth muscle and is neuroprotective against glutamate NMDA toxicity.PPADS tetrasodiuma inhibits P2X1, P2X-2, P2X-3, and P2X- 5. 5.

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