2. シグナル伝達
  3. Membrane Transporter/Ion Channel
  4. P2X Receptor

P2X Receptor

P2XRs

P2X Receptor

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P2X receptors are a family of seven (P2X1R-P2X7R) cation permeable ligand-gated ion channels (LGICs) that open in response to binding by the extracellular ligand, adenosine 5′-triphosphate (ATP). P2X receptors have a high permeability to Ca2+, Na+, and K+ and are expressed widely throughout the nervous, immune, cardiovascular, skeletal, gastrointestinal, respiratory, and endocrine systems.

P2X receptors are widely expressed in excitatory and non-excitatory cells, such as neuron, glia, platelet, epithelia and macrophage, and participate in many important physiological and pathological processes, including synaptic transmission, pain perception, inflammation, cardiovascular modulation, immunomodulation and tumorigenesis.

P2X Receptor Isoform Specific Products:

P2X Receptor Isoform Comparison
製品番号 製品名 製品効果 純度 構造式
  • HY-150270
    NP-1815-PX Antagonist
    NP-1815-PX is an orally active dual inhibitor of P2X4 and prostaglandin TP receptors, with an IC50 of 0.26 μM against human P2X4 receptors. NP-1815-PX specifically inhibits ATP-mediated prostaglandin production, TP receptor-induced calcium elevation, and the canonical/non-canonical NLRP3 inflammasome signaling pathway. NP-1815-PX selectively blocks smooth muscle contractions induced by ATP, U46619 (HY-108566) and prostaglandin F2α. NP-1815-PX not only produces anti-allodynic effects in vivo, but also significantly alleviates symptoms of DNBS (HY-W324435)-induced colitis (such as weight loss and tissue damage). NP-1815-PX exerts anti-inflammatory effects by downregulating IL-1β levels and Caspase-1 activity. NP-1815-PX is used in studies related to asthma and inflammatory bowel disease (colitis).
    NP-1815-PX
  • HY-179373
    UB-MBX-46 Antagonist
    UB-MBX-46 is a potent and selective P2X7 receptor antagonist with IC50s of 0.514 nM (hP2X7R), 40.6 nM (rP2X7R), and 4.52 nM (mP2X7R), respectively. UB-MBX-46 interacts with the classical allosteric pocket of the human P2X7 receptor. UB-MBX-46 can be used for cancer, atherosclerosis, and neurode generation research.
    UB-MBX-46
  • HY-108960
    PPADS Antagonist
    PPADS is a P2X receptor (P2X Receptor) antagonist and a reversible competitive antagonist of NAADP receptors, with IC50 values of 68 nM (P2X1) and 214 nM (P2X3), respectively. PPADS alleviates pain-related behaviors in the central and peripheral nervous systems of mice after peripheral neuropathy, inhibits the overproduction of IL-1β, IL-6, iNOS and nNOS, and suppresses the hydrolytic activity of extracellular ATPase. PPADS blocks ATP-mediated inward currents on recombinant rat P2X1 and P2X3 receptors, and inhibits purinergic nerve stimulation-induced contraction of rabbit bladder detrusor muscle. PPADS is applicable to research related to neuropathic pain.
    PPADS
  • HY-178450
    HW091077 Inhibitor
    HW091077 is a highly selective P2X3 receptor antagonist with an IC50 of 17 nM. HW091077 blocks ATP-induced calcium influx and cell depolarization to inhibit cough reflex pathways. HW091077 is promising for research of chronic cough.
    HW091077
  • HY-175196
    P2X7 receptor antagonist-6 Antagonist
    P2X7 receptor antagonist-6 (Compound 2g) is a negative allosteric P2X7 receptor antagonist with an IC50 of 1.31  μM for hP2X7. P2X7 receptor antagonist-6 can be used for cancer, neurodegenerative, inflammatory, and infectious diseases research.
    P2X7 receptor antagonist-6
  • HY-134440
    α,β-Methylene-ATP dilithium Agonist
    α,β-Methylene-ATP dilithium is an agonist of P2X1 and P2X3 receptors and can cross the blood-brain barrier. α,β-Methylene-ATP dilithium can trigger a reflex pressor response by activating P2X receptors in peripheral muscles and the central locus coeruleus (LC); this effect can be blocked by the P2X antagonist PPADS (HY-108960). α,β-Methylene-ATP dilithium also activates noradrenergic neurons in the central locus coeruleus, mediating antinociceptive effects; this effect can be attenuated by the locus coeruleus damaging agent DSP-4 (HY-103210/HY-121602). α,β-Methylene-ATP dilithium can be used to study the pathological mechanisms of neuropathic pain, cardiovascular reflex regulation, and antinociceptive effects of the central nervous system.
    α,β-Methylene-ATP dilithium
  • HY-19427
    AZD9056 Antagonist
    AZD9056 is a P2X7 purinergic receptor antagonist with anticancer activity. AZD9056 can inhibit the invasion and metastasis of cancer stem cells.
    AZD9056
  • HY-101588AR
    Gefapixant citrate (Standard) Antagonist
    Gefapixant (citrate) (Standard) is the analytical standard of Gefapixant (citrate) (HY-101588A). This product is intended for research and analytical applications. Gefapixant citrate is an orally active and potent purinergic P2X3 receptor (P2X3R) antagonist, with IC50 values of ~30 nM versus recombinant hP2X3 homotrimers and 100-250 nM at hP2X2/3 heterotrimeric receptors. Gefapixant citrate can be used for the research of chronic cough and knee osteoarthritis.
    Gefapixant citrate (Standard)
  • HY-134370
    Ap4G
    Ap4G is a dinucleoside polyphosphate compound with vasoconstrictor activity. Ap4G regulates vasoconstriction through P2 receptors, especially P2X receptors, and is an important tool for studying vascular physiology and pathology.
    Ap4G
  • HY-101911R
    5-BDBD (Standard) Antagonist
    5-BDBD (Standard) is the analytical standard of 5-BDBD (HY-101911). This product is intended for research and analytical applications. 5-BDBD, a potent and selective P2X4 receptor antagonist, inhibits rP2X4R-mediated currents, with an IC50 of 0.75 μM. 5-BDBD completely blocks the basal and acute hyperalgesia induced by nitroglycerin (NTG).
    5-BDBD (Standard)
  • HY-129731
    Lappaconine Inhibitor
    Lappaconine is a diterpenoid alkaloid. Lappaconine can be used for α-hydroxylation of β-oxo esters.
    Lappaconine
  • HY-122272S
    Paroxetine-d4 Inhibitor
    Paroxetine-d4 (BRL29060-d4) is deuterium labeled Paroxetine. Paroxetine is an oral inhibitor that falls under the category of selective serotonin reuptake inhibitors (SSRIs). Paroxetine is also a very weak norepinephrine (NE) reuptake inhibitor, capable of inducing cell apoptosis and having anti-tumor activity. Paroxetine has antidepressant, anti-anxiety, and pain-relieving effects, and it can help improve conditions like obsessive-compulsive disorder, panic disorder, post-traumatic stress disorder, premenstrual anxiety, and chronic headaches.
    Paroxetine-d<sub>4</sub>
  • HY-101910R
    PSB-12062 (Standard) Antagonist
    PSB-12062 (Standard) is the analytical standard of PSB-12062 (HY-101910). This product is intended for research and analytical applications. PSB-12062 is a potent and selective P2X4 antagonist with an IC50 of 1.38 μM for human P2X4.
    PSB-12062 (Standard)
  • HY-15488AR
    A 438079 hydrochloride (Standard) Antagonist
    A 438079 (hydrochloride) (Standard) is the analytical standard of A 438079 (hydrochloride). This product is intended for research and analytical applications. A 438079 (hydrochloride) is a potent, and selective P2X7 receptor antagonist with pIC50 of 6.9.
    A 438079 hydrochloride (Standard)
  • HY-15488R
    A 438079 (Standard) Antagonist
    A 438079 (Standard) is the analytical standard of A 438079. This product is intended for research and analytical applications. A 438079 is a potent, and selective P2X7 receptor antagonist with pIC50 of 6.9.
    A 438079 (Standard)
  • HY-183056
    P2X3 antagonist 40 Antagonist
    P2X3 antagonist 40 is a P2X3 antagonist with a human P2X3 receptor pIC50 < 4.52. P2X3 antagonist 40 can be used for research on ATP-mediated proinflammatory fingerprint, including overactive bladder, pain, and chronic cough.
    P2X3 antagonist 40
  • HY-14483R
    AF-353 (Standard) Antagonist
    AF-353 (Standard) is the analytical standard of AF-353. This product is intended for research and analytical applications. AF-353 (Ro-4) is a potent, selective and orally bioavailable P2X3/P2X2/3 receptor antagonist, with a pIC50 of 8.0 for both human and rat P2X3, and with a pIC50 of 7.3 for human P2X2/3.
    AF-353 (Standard)
  • HY-N1478R
    Gardenoside (Standard)
    Gardenoside is an orally active natural compound found in Gardenia fruits. Gardenoside reliefs chronic constriction injury (CCI)-induced neuropathic pain by regulating the P2X3 and P2X7 receptors. Gardenoside has an inhibitory effect on free fatty acids (FFA)-induced cellular steatosis. Gardenoside reduces reactive oxygen species (ROS). Gardenoside can be used for anti-inflammatory, antinociceptive and hepatoprotective study.
    Gardenoside (Standard)
  • HY-108669R
    AZ10606120 dihydrochloride (Standard) Antagonist
    AZ10606120 dihydrochloride (Standard) is the analytical standard of AZ10606120 (dihydrochloride) (HY-108669). This product is intended for research and analytical applications. AZ10606120 dihydrochloride is a selective, high affinity antagonist for P2X7 receptor (P2X7R) at human and rat with an IC50 of about 10 nM. AZ10606120 dihydrochloride is little or no effect at other P2XR subtypes. AZ10606120 dihydrochloride has anti-depressant effects and reduces tumour growth.
    AZ10606120 dihydrochloride (Standard)
  • HY-15470
    GW791343 trihydrochloride Inhibitor
    GW791343 trihydrochloride is a potent human P2X7 receptor negative allosteric modulator (exhibits species-specific activity), produces a non-competitive antagonist effect on human P2X7 receptor, with a pIC50 of 6.9-7.2. GW791343 trihydrochloride can enhance ATP rhythm. GW791343 trihydrochloride can be used in study of neurological disease.
    GW791343 trihydrochloride
P2X Receptor Isoform Comparison

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