Catalog No.
Product Name
Application
Product Information
Citations
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P2X3 Receptor Inhibitor
P2X3-IN-1 is a selective inhibitor of the P2X3 receptor, which plays a crucial role in mediating pain and other neurogenic responses. This compound demonstrates significant biological activity in modulating P2X3 receptor signaling, making it valuable for research into neurogenic diseases and pain pathways. Researchers can utilize P2X3-IN-1 to explore therapeutic strategies for conditions associated with P2X3 receptor dysfunction. -
P2X3/P2X2/3 Receptor Antagonist
RO-3 is a potent orally active antagonist of the P2X3 and P2X2/3 receptors, exhibiting pIC50 values of 5.9 and 7.0 for human homomultimeric P2X3 and heteromultimeric P2X2/3 receptors, respectively. This compound demonstrates selectivity for P2X3 and P2X2/3, with IC50 values exceeding 10 μM against all other functional P2X receptor homomultimers, including P2X1, P2X2, P2X4, P2X5, and P2X7. RO-3 is valuable for research focused on pain pathways and chronic pain conditions due to its specific receptor interactions. -
P2X Agonist
BzATP triethylammonium is a potent P2X receptor agonist that exhibits varying pEC50 values across multiple P2X receptor subtypes, including 8.74 for P2X1, 5.26 for P2X2, 7.10 for P2X3, 7.50 for P2X2/3, 6.19 for P2X4, and 6.31 for P2X7. It demonstrates significant activity at P2X7 receptors, with EC50 values of 3.6 μM for rat P2X7 and 285 μM for mouse P2X7. BzATP triethylammonium is valuable for research investigating purinergic signaling pathways and receptor pharmacology. -
P2X4 Inhibitor
P2X4 antagonist-1 is a potent inhibitor of the P2X4 receptor, exhibiting an IC50 of 15 nM. This compound effectively modulates P2X4 signaling, making it valuable for research involving pain modulation, neuroinflammation, and cardiovascular regulation. Its specificity towards P2X4 supports studies aimed at understanding its role in various pathophysiological conditions. -
P2X1 receptor antagonist
Ro 0437626 is a selective antagonist of the purinergic P2X1 receptor, exhibiting an IC50 value of 3 μM. It demonstrates low affinity for P2X2, P2X3, and P2X2/3 receptors, with IC50 values exceeding 100 μM. This compound is valuable for research applications involving the modulation of P2X1 receptor signaling pathways, contributing to studies in cardiovascular and pain research. -
P2X7 Receptor Antagonists
AZ 11645373 is a selective antagonist of the human P2X7 receptor, demonstrating significant potency without affecting the rat variant. It effectively inhibits ATP-induced release of IL-1β from lipopolysaccharide-activated THP-1 cells, with an IC50 value of 90 nM. This compound is valuable for studies focused on inflammatory processes and purinergic signaling pathways. -
P2X4 Receptor Antagonist
MRS4719 is a potent antagonist of the P2X4 receptor, exhibiting an IC50 value of 0.503 μM in human P2X4 receptor assays. This compound demonstrates neuroprotective effects by reducing infarct volume and promoting neurorehabilitation in models of ischemic stroke. Additionally, MRS4719 effectively decreases ATP-induced intracellular calcium influx in primary human monocyte-derived macrophages, making it a valuable reagent for studying ischemic stroke and related neuroinflammatory processes. -
P2X Receptor Antagonist
AF-353 hydrochloride is a potent and selective antagonist of the P2X3 and P2X2/3 receptors, exhibiting a pIC50 of 8.0 for both human and rat P2X3 and a pIC50 of 7.3 for human P2X2/3. This compound is notable for its oral bioavailability, making it suitable for in vivo studies. AF-353 hydrochloride is primarily utilized in research applications focused on pain modulation and the study of purinergic signaling pathways. -
P2X3 Antagonist
P2X3 antagonist 38 is a potent oral antagonist of the P2X3 receptor, demonstrating IC50 values of 0.132 µM for human P2X3, 0.165 µM for rat P2X3, and 0.421 µM for guinea pig P2X3. This compound is valuable in studies focused on pain modulation and respiratory disorders, positioning it as a significant tool for researching the role of P2X3 in various biological processes. Its high selectivity and efficacy make it suitable for in vivo applications in pharmacological investigations. -
P2X3 Receptor Inhibitor
Purotoxin 1 is a selective P2X3 receptor inhibitor. It exhibits significant antinociceptive effects in animal models of inflammatory pain, making it a valuable tool for pain research. Isolated from the venom of the wolf spider Geolycosa sp., Purotoxin 1 can be utilized in studies aimed at understanding pain mechanisms and developing new analgesic therapies. -
P2X7 Antagonist
(S)-JNJ-54166060 is a selective P2X7 antagonist, exhibiting potent inhibitory activity against the P2X7 receptor. This compound is useful in research related to chronic inflammatory diseases, neurodegeneration, and pain pathways, as well as studying the role of P2X7 in immune responses. Its specificity and efficacy make it a valuable tool for investigating the therapeutic potential of modulating P2X7 signaling. -
P2X1 Receptor Inhibitor
NF864 is a selective inhibitor of the P2X1 receptor, primarily expressed in human platelets. This compound effectively disrupts ATP-mediated signaling cascades involved in platelet activation and aggregation. NF864 is useful in research applications focused on cardiovascular disease, thrombosis, and platelet-related disorders, allowing scientists to investigate the role of P2X1 in vascular biology. -
P2X4 Receptor Antagonist
MRS4596 is a potent and selective antagonist of the P2X4 receptor, exhibiting an IC50 value of 1.38 μM for the human P2X4 receptor. This compound demonstrates neuroprotective and neuro-rehabilitative effects in models of ischemic stroke. MRS4596 is applicable in the study of ischemic stroke and associated therapeutic strategies. -
P2X-Purinoceptor Antagonist
Iso-PPADS tetrasodium is a selective antagonist of the P2X purinoceptors, specifically targeting P2X1 and P2X3 receptors with IC50 values of 43 nM and 84 nM, respectively. This compound is known for its neuroprotective effects, particularly in the context of ventilator-induced brain injury (VIBI). Iso-PPADS tetrasodium is useful for researchers investigating purinergic signaling pathways and their implications in various neurological conditions. -
P2X7 Receptor Antagonist
JNJ-54166060 is a potent and selective antagonist of the P2X7 receptor, exhibiting IC50 values of 4 nM for the human, 115 nM for the rat, and 72 nM for the mouse P2X7 receptor. This compound modulates the purinergic signaling pathway, influencing processes such as inflammation and cell death. JNJ-54166060 is valuable for research applications related to autoimmune diseases, neuroinflammation, and other conditions where P2X7 receptor modulation is of interest. -
P2X4 Antagonist
P2X4 antagonist-2 is a selective antagonist of the P2X4 purinergic receptor, exhibiting an IC50 of 24 nM. This compound effectively inhibits ATP-induced P2X4 receptor activation, providing valuable insights into the role of P2X4 in various physiological and pathological processes. It is suitable for research focused on inflammation, pain signaling, and neurobiology. -
P2X Antagonist
Relicpixant is a potent antagonist of the purinergic P2X receptor family. It has been shown to effectively inhibit P2X receptor-mediated signaling pathways, making it valuable for studying the role of purinergic signaling in various physiological and pathological processes. This compound is applicable in research areas such as neurobiology, pain modulation, and inflammation, where P2X receptors play critical roles. -
P2X4 Inhibitor
P2X4-IN-1 is a potent inhibitor of the P2X4 receptor, which is involved in various physiological processes including pain perception and inflammation. This compound demonstrates significant biological activity by selectively blocking P2X4 receptor signaling. Its application in research allows for the investigation of therapeutic strategies for diseases associated with P2X4 receptor dysregulation. -
P2X3 Receptor Antagonist
P2X3 antagonist 37 is a selective antagonist of the P2X3 receptor, exhibiting an inhibitory concentration (IC50) of 32.45 nM for human P2X3. This compound interrupts ATP-mediated signaling, making it a valuable tool for research into pain pathways and bladder dysfunction. It supports investigations exploring P2X3 receptor roles in neurobiology and related therapeutic applications. -
P2X(3)/P2X(2/3) Antagonist
Ro-51 is a selective antagonist of the P2X3 and P2X2/3 receptors, demonstrating IC50 values of 2 nM and 5 nM, respectively. This compound effectively inhibits ATP-mediated signaling through these receptors, making it a valuable tool in pain research. Its specificity and potency allow for detailed investigations into the role of purinergic signaling in nociception and associated pain pathways. -
P2X3 Antagonist
P2X3 antagonist 36 is a potent antagonist of the P2X3 receptor, which plays a critical role in the modulation of pain and sensory signaling. This compound effectively inhibits P2X3 activity, making it a valuable tool for exploring the mechanisms underlying pain pathways. It is particularly useful in research focused on pain management and the development of analgesic therapies. -
ATP Analogue
8-Bromo-ATP, an ATP analogue, serves as a potent agonist for purinergic P2X receptors. This compound demonstrates cytotoxic effects on multiple myeloma cells, with an IC50 value of 23.1 μM, highlighting its potential for cancer research. 8-Bromo-ATP is useful in studies investigating purinergic signaling and its implications in tumor biology. -
P2X Receptor Antagonist
P2X7 receptor antagonist-5 is a potent inhibitor of the P2X7 receptor, a crucial target in various inflammatory and neurological disorders. This compound is characterized by its oral bioavailability and prolonged action, making it suitable for in vivo studies. It holds potential for applications in researching pain, neurodegeneration, and immune responses linked to P2X7 receptor signaling. -
P2X7 Receptor Antagonist
P2X7 receptor antagonist-3 is a highly potent antagonist of the P2X7 receptor, demonstrating IC50 values of 4.2 nM in human cells and 6.8 nM in rat models. This compound inhibits the activation of the P2X7 receptor, which is involved in inflammatory responses and various signaling pathways. It is suitable for research applications focused on pain, neuroinflammation, and autoimmune diseases, enabling the exploration of therapeutic strategies targeting P2X7 receptor-mediated mechanisms. -
P2X7 Receptor Inhibitor
GSK1370319A is a selective inhibitor of the human P2X7 receptor, demonstrating an IC50 of 474 nM and a Ki of 176 nM. This compound effectively inhibits the production of interleukin-1 beta (IL-1β), decreases the generation of reactive oxygen species (ROS), and enhances macrophage survival rates. GSK1370319A is applicable in research related to inflammatory bowel disease and the broader study of inflammatory processes. -
P2X Receptor Inhibitor
P2X receptor-1 is a selective inhibitor of P2X receptors, which play a critical role in mediating pain and inflammatory responses. This compound has potential applications in research focused on understanding nociception and addressing inflammatory conditions. Its ability to modulate P2X receptor activity makes it an important tool for exploring therapeutic strategies in pain management and inflammation research. -
Probe of P2X1 Receptor
MRS 2219 is a selective pharmacological probe for the P2X1 receptor, primarily functioning as an antagonist. It enhances ATP-evoked responses at P2X1 receptors with an EC50 of 5.9 μM, making it essential for studies involving purinergic signaling in cardiovascular and neurological research. This compound is particularly valuable for elucidating the role of P2X1 receptors in various physiological processes and pathological conditions. -
P2X1/3 Receptor Agonist
α,β-Methylene-ATP is a selective agonist of the P2X1 and P2X3 receptors, capable of crossing the blood-brain barrier. Its activation of P2X receptors induces a reflex pressor response associated with the peripheral muscles and the central locus coeruleus, while engaging noradrenergic neurons that mediate antinociceptive effects. α,β-Methylene-ATP is a valuable tool for investigating neuropathic pain mechanisms, cardiovascular reflex regulation, and the central nervous system's antinociceptive pathways. -
P2X2/3 Modulator
P2X2/3 modulator-1 is a selective modulator targeting the P2X2 and P2X3 purinergic receptors. This compound exhibits significant biological activity in the modulation of pain pathways and inflammation processes. It is applicable in research focused on pain management, central nervous system disorders, and inflammatory conditions, providing insights into therapeutic strategies for these ailments. -
P2X4R Antagonist
NP-1815-PX is a selective antagonist of the P2X4 receptor, demonstrating potent inhibition of this target. It exhibits significant anti-inflammatory properties and has been shown to alleviate pain in chronic pain models. Additionally, NP-1815-PX effectively inhibits contractions in guinea pig tracheal and bronchial smooth muscle, making it a valuable tool for research in respiratory and pain-related studies. -
P2X3 Receptor Antagonist
HW091077 is a selective antagonist of the P2X3 receptor, exhibiting an IC50 of 17 nM. By inhibiting ATP-induced calcium influx and preventing cell depolarization, HW091077 effectively disrupts cough reflex pathways. This compound holds potential for research applications focused on chronic cough mechanisms. -
P2X7 Receptor Antagonist
P2X7 receptor antagonist-6 is a negative allosteric modulator targeting the P2X7 receptor, exhibiting an IC50 of 1.31 μM for human P2X7. This compound demonstrates potential for research applications in cancer, neurodegenerative disorders, inflammatory responses, and infectious diseases, contributing to a greater understanding of P2X7's role in these conditions. Its specificity and efficacy make it a valuable tool for exploring therapeutic pathways in related research fields. -
P2X1,3-Selective Agonist
α,β-Methylene-ATP dilithium is a selective agonist for P2X1 and P2X3 receptors, capable of crossing the blood-brain barrier. It induces a reflex pressor response by activating these receptors in peripheral muscles and the central locus coeruleus, with effects that can be inhibited by the P2X antagonist PPADS. Additionally, it stimulates noradrenergic neurons in the central locus coeruleus, contributing to antinociceptive effects that can be reduced by DSP-4. This compound is valuable for investigating the mechanisms underlying neuropathic pain, cardiovascular reflex regulation, and central nervous system analgesia. -
P2X7 Purinergic Receptor Antagonist
AZD9056 is a potent antagonist of the P2X7 purinergic receptor, which plays a significant role in cancer progression. This compound exhibits notable anticancer activity by inhibiting the invasion and metastasis of cancer stem cells. As a result, AZD9056 is valuable for research focused on cancer biology and novel therapeutic strategies targeting purinergic signaling pathways. -
Vasoconstrictor
Ap4G is a dinucleoside polyphosphate that functions as a vasoconstrictor by modulating P2 receptors, particularly P2X receptors. This compound is instrumental for research into vascular physiology and pathology, providing insights into mechanisms of vasoconstriction and related cardiovascular conditions. Its distinct biological activity makes it a valuable reagent for studies investigating the role of purinergic signaling in vascular health. -
P2X7 Antagonist
ITH15004 is a potent antagonist of the P2X7 receptor, effectively penetrating the central nervous system. This compound is utilized in research focused on neurodegenerative diseases, providing insights into the role of ATP-gated ion channels in neuroinflammation and neuronal cell death. Its ability to modulate P2X7 receptor activity makes it a valuable tool in understanding therapeutic strategies for neurological disorders. -
P2X1 Receptor Antagonist
NF449 is a potent antagonist of the P2X1 receptor, demonstrating IC50 values of 0.28 nM for rP2X1, 0.69 nM for rP2X1+5, and 120 nM for P2X2+3. It selectively inhibits Gsα coupling, suppressing GTP[γS] binding to Gsα-s and diminishing adenylyl cyclase activity. This compound is crucial for research applications involving the modulation of purinergic signaling and studies related to cardiovascular and inflammatory conditions. -
P2X Receptor Control
P2X4 antagonist-5 is a selective antagonist for the P2X4 receptor, exhibiting an IC50 greater than 100 μM in human P2X4 assays. This compound serves as a control in studies investigating the modulation of P2X4 receptor activity. It is useful for researchers examining the role of purinergic signaling in various physiological and pathological processes. -
P2X3 Inhibitor
TC-P 262 is a highly effective inhibitor of the P2X3 receptor, a key player in pain and inflammatory responses. By binding to the human P2X3 receptor, TC-P 262 demonstrates significant inhibitory effects, making it a valuable tool for studying conditions such as rheumatoid arthritis, chronic cough, and pain management. This reagent facilitates the exploration of P2X3's role in these biological processes, contributing to the understanding of potential therapeutic interventions. -
P2X Receptor Antagonist
PPADS tetrasodium is a non-selective antagonist of P2X receptors, effectively inhibiting recombinant P2X1, -2, -3, and -5 with IC50 values ranging from 1 to 2.6 μM. Additionally, it shows inhibitory effects on native P2Y2-like receptors (IC50 ~0.9 mM) and recombinant P2Y4 receptors (IC50 ~15 mM). This compound also acts as an inhibitor of the reverse mode of the Na/Ca2+ exchanger in guinea pig airway smooth muscle, making it a valuable tool for research on purinergic signaling and related physiological processes. -
P2X4 Receptor Antagonist
BX430 is a potent noncompetitive allosteric antagonist of the human P2X4 receptor, exhibiting an IC50 value of 0.54 μM. This compound demonstrates selectivity and species specificity, making it a valuable tool for investigating the role of P2X4 receptors in various biological processes. BX430 is primarily utilized in research applications related to chronic pain and cardiovascular diseases, providing insight into therapeutic potential in these areas. -
Calcium Channel
2-Chloro-ATP sodium is an analog of ATP that acts as an antagonist of the purinergic P2Y1 receptor, inhibiting intracellular calcium mobilization induced by ADP in Jurkat cells with a Ki of 2.3 μM. Additionally, it serves as an agonist for the purinergic P2X receptor, generating inward currents in HEK293 cells with varying affinities (EC50 of 0.5 and 2.5 μM). This compound also induces concentration-dependent relaxation of precontracted guinea pig cecal strips. Furthermore, 2-Chloro-ATP sodium is utilized to investigate substrate specificity among cyclic nucleotide-dependent protein kinases, including protein kinase A (PKA) and PKG. -
Antispastic Agent, Muscle Relaxant, P2X7 Receptor Antagonist
Eperisone hydrochloride primarily acts as a P2X7 receptor antagonist and is recognized for its antispastic and muscle relaxant properties. This compound is effective in alleviating muscle stiffness and pain, showcasing vasodilatory effects. In addition to its action on skeletal muscles, Eperisone hydrochloride also exhibits antagonistic effects on human P2X3 receptors, contributing to improved circulation and the suppression of myotonia-related pain reflexes, making it valuable for muscle-related research applications.
