Catalog No.
Product Name
Application
Product Information
Citations
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P2X7 modulator
GW791343 HCl acts as a negative allosteric modulator of human P2X7 (pIC50 = 6.9 - 7.2) and a positive allosteric modulator of rat P2X7. - Ticlopidine is an adenosine diphosphate (ADP) receptor inhibitor. It inhibits platelet aggregation by altering the function of platelet membranes by blocking ADP receptors. This prevents the conformational change of glycoprotein IIb/IIIa which allows platelet binding to fibrinogen.
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P2X3 and P2X2/3 receptor antagonist
A-317491 sodium salt hydrate is a non-nucleotide P2X3 and P2X2/3 receptor antagonist, which inhibits calcium flux mediated by the receptors. -
P2X7 receptor antagonist
A-438079 HCl is a competitive P2X7 receptor antagonist (pIC50 = 6.9 for the inhibition of Ca2+ influx in the human recombinant P2X7 cell line). Devoid of activity at other P2 receptors (IC50 >> 10 uM). -
P2X7 receptor antagonist
A 438079 Hcl is a competitive P2X7 receptor antagonist (pIC50 = 6.9 for the inhibition of Ca2+ influx in the human recombinant P2X7 cell line).- Zhihua Yi, .et al. , Front Pharmacol, 2018, 9: 593 PMID: 29950989
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hepatoprotective agent
Gardenoside is a natural compound found in Gardenia fruits, with hepatoprotective properties. Gardenoside suppresses the pain of chronic constriction injury by regulating the P2X3 and P2X7 receptors. Gardenoside has an inhibitory effect on free fatty acids (FFA)-induced cellular steatosis. -
P2X7 receptor antagonist
JNJ-54175446 is a potent and selective brain penetrant P2X7 receptor antagonist, with pIC50s of 8.46 and 8.81 for hP2X7 receptor and rP2X7 receptor, respectively. -
P2X3R antagonist
Gefapixant is an orally active P2X3 receptor (P2X3R) antagonist with IC50s of ~30 nM versus recombinant hP2X3 homotrimers and 100-250 nM at hP2X2/3 heterotrimeric receptors. -
P2X7R antagonist
AZ10606120 dihydrochloride is a selective, high affinity antagonist for P2X7 receptor (P2X7R) at human and rat with an IC50 of ~10?nM. -
P2X7 allosteric modulator
GW791343 3Hcl is a P2X7 allosteric modulator; exhibits species-specific activity and acts as a negative allosteric modulator of human P2X7 (pIC50 = 6.9 - 7.2). -
purinergic P2X2/3 receptors antagonist
Minodronic acid (YM-529) is an antagonist of purinergic P2X2/3 receptors involved in pain. -
P2X7 receptor antagonist
NSC 102533 is a potent antagonist of the purinergic P2X7 receptor, a ligand-gated ion channel involved in inflammation and immune regulation. It effectively inhibits ATP-induced dye uptake in HEK293 cells expressing human P2X7 receptors with an IC₅₀ of 22.4 nM. NSC 102533 also suppresses ATP-induced IL-1β secretion in human THP-1 monocytes and primary mouse peritoneal macrophages, with IC₅₀ values of 9.8 nM and 11.2 nM, respectively, demonstrating strong anti-inflammatory activity.
In addition to its immunomodulatory effects, NSC 102533 exhibits antivenom potential by inhibiting Bothrops atrox venom proteolysis in a concentration-dependent manner. In in vivo studies, intradermal administration of NSC 102533 (3 mg/kg) significantly reduces skin hemorrhage induced by B. atrox and B. jararaca venom and attenuates carrageenan-induced paw edema in mice at doses between 0.01 and 1 mg/kg. These properties highlight NSC 102533 as a valuable pharmacological tool for studying P2X7 receptor–mediated inflammatory responses and venom-induced pathology.
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P2X7 Antagonist
Bullatine A is a potent P2X7 antagonist with significant anti-inflammatory and anti-nociceptive properties. It effectively inhibits ATP-induced BV-2 cell apoptosis and modulates inflammatory responses mediated by P2X receptors. Bullatine A has demonstrated the ability to reduce glioma cell growth by targeting SIRT6, alleviate pain hypersensitivity in rodent models, and mitigate systemic inflammation via the ROS/JNK/NF-κB pathway. Additionally, it has shown potential in improving behavioral outcomes in models of chronic social defeat stress. This compound is valuable for research in inflammation, glioblastoma, and depression. -
P2X2/3 Receptor Antagonist
Minodronic acid hydrate is a third-generation bisphosphonate that acts as an antagonist of the purinergic P2X2/3 receptors. It demonstrates the ability to inhibit the proliferation of cancer cells, induce apoptosis, and restrict metastasis in various cancer types. This compound is particularly relevant in pain research, providing insights into its role in managing nociception associated with P2X2/3 receptor activity. -
P2X7 Modulator
GSK-1482160 is a negative allosteric modulator of the P2X7 receptor (P2X7R), with high oral bioavailability and the ability to penetrate the blood-brain barrier. It has demonstrated a human pIC50 of 8.5 and a rat pIC50 of 6.5, effectively reducing ATP's efficacy at the receptor without altering its affinity, which subsequently inhibits IL-1β release. This compound serves as a valuable radioligand for P2X7R imaging using isotopes such as 11C or 18F and is applicable in research related to chronic joint pain and chronic constriction injury (CCI). -
P2X7R Activitor
HEI3090 is a potent P2X7 receptor (P2X7R) activator. It effectively stimulates dendritic cells that express P2X7R to release IL-18, promoting the activation of Natural Killer cells and CD4 T cells. This cascade results in increased production of IFN-γ, thereby fostering a sustained antitumor immune response. HEI3090 is particularly beneficial in enhancing the efficacy of αPD-1 therapy for non-small cell lung cancer (NSCLC). -
P2X7 Receptor Inhibitor
P2X7-IN-2 is a potent inhibitor of the P2X7 receptor, demonstrating an IC50 value of 0.01 nM for the inhibition of IL-1β release. This compound is valuable in research focusing on the mechanisms of autoimmunity, inflammation, and cardiovascular disease. Its selective action on the P2X7 receptor makes it a critical tool for studying inflammatory pathways and potential therapeutic interventions. -
P2 receptor/NAADP receptor Antagonist
PPADS is a reversible competitive antagonist of P2X receptors, specifically targeting P2X1 and P2X3, with IC50 values of 68 nM and 214 nM, respectively. It demonstrates significant anti-nociceptive effects in mouse models of neuropathic pain and inhibits pro-inflammatory cytokines such as IL-1β and IL-6, as well as nitric oxide synthases. Additionally, PPADS effectively blocks ATP-mediated inward currents in recombinant rat P2X receptors and reduces contractions in rabbit bladder detrusor muscle induced by purinergic nerve stimulation. This compound is valuable for research on neuropathic pain mechanisms and related therapeutic interventions. -
P2X7R Selective Allosteric Antagonist
SMW139 is a selective allosteric antagonist of the P2X7 receptor, demonstrating a Ki value of 32 nM for human P2X7R. This compound exhibits potential in modulating inflammatory responses and has applications in research related to Alzheimer's disease and multiple sclerosis. With a half-life of 47 minutes in rat liver microsomes, SMW139 serves as a valuable tool for investigating the therapeutic effects on P2X7R-mediated pathways. -
P2X1 Receptor Activator
Diadenosine pentaphosphate (pentasodium) is an agonist and negative modulator of the P2X1 receptor, an important endogenous purine dinucleotide primarily sourced from platelets. This compound is known to negatively regulate dendritic growth and branching by activating both homologous and heterologous P2X1 receptors, resulting in a modest transient increase in intracellular calcium levels in dendritic growth cones. Diadenosine pentaphosphate demonstrates selective inhibition of dendrite growth in cultured hippocampal neurons while leaving axon growth unaffected. Its presence in secretory vesicles such as platelets and brain synaptosomes highlights its biological relevance in neurophysiological studies. -
P2X4 Antagonist
PSB-12054 is a selective antagonist of the P2X4 receptor, exhibiting an IC50 of 0.189 μM in human P2X4 assays. This compound has significant potential for studying neuropathic pain mechanisms and exploring therapeutic strategies for neurodegenerative diseases. Its specificity for P2X4 makes it a valuable tool for researchers investigating purinergic signaling pathways. -
P2X Receptor Inhibitor
PSFL2915 is a selective inhibitor of the P2X receptor family, exhibiting an IC50 of 0.319 μM for human P2X3 and 0.261 μM for rat P2X2/3, with approximately 42-fold selectivity for human P2X3 over human P2X2. This compound inhibits human P2X3 activation by disrupting the allosteric tightening of the inner pocket necessary for channel opening, with dependency on magnesium for its inhibitory effect. Additionally, PSFL2915 demonstrates inhibitory activity against rat P2X2/3 and human P2X2 receptors, while showing minimal effects on human P2X1, P2X4, and P2X7 receptors. It is applicable in chronic cough research. -
P2X4 Receptor Antagonist
5-BDBD is a selective antagonist of the P2X4 receptor, demonstrating potent inhibition of rP2X4R-mediated currents with an IC50 of 0.75 μM. This compound effectively interferes with both basal and acute hyperalgesia induced by nitroglycerin (NTG). 5-BDBD is valuable for studying pain mechanisms and the role of purinergic signaling in nociception. -
P2X3/P2X7 Receptor Ligand
α,β-Methylene-ATP trisodium is a potent agonist of P2X3 and P2X7 receptors, which facilitates significant biological responses through purinergic receptor activation. This compound is capable of traversing the blood-brain barrier, thereby influencing both peripheral and central nervous system pathways. It is instrumental in studying reflex cardiovascular responses and antinociceptive mechanisms mediated by noradrenergic neurons in the locus coeruleus. Researchers utilize α,β-Methylene-ATP trisodium for insights into neuropathic pain mechanisms and cardiovascular reflex regulation. -
P2X4 Antagonist
BAY-1797 is a selective antagonist of the P2X4 receptor, demonstrating a potent inhibition with an IC50 of 211 nM in human P2X4 assays. This compound exhibits minimal activity toward other P2X ion channels, allowing for targeted research applications. BAY-1797 has been shown to provide anti-nociceptive and anti-inflammatory effects, making it a valuable tool for studies into pain modulation and inflammatory processes. -
P2X Receptor Inhibitor
AZD9056 hydrochloride is a selective oral inhibitor of the P2X7 receptor, which is implicated in various inflammatory and pain-related conditions. By blocking P2X7 activity, this compound demonstrates potential in modulating inflammatory responses, making it a valuable tool for research in pain management and inflammatory disease pathways. Its application in preclinical studies may help elucidate the role of purinergic signaling in various biological processes. -
P2X7 Antagonist
JNJ-47965567 is a high-affinity, selective antagonist of the P2X7 receptor, exhibiting centrally permeable properties with pKis of 7.9 for human P2X7 and 8.7 for rat P2X7. This compound is instrumental in investigating the role of central P2X7 in rodent models, providing insights into its involvement in various CNS pathophysiological conditions. JNJ-47965567 is valuable for studies aimed at elucidating the molecular mechanisms underlying neurological disorders. -
P2X3 Antagonist
Camlipixant is a potent, selective, non-competitive antagonist of the P2X3 receptor, exhibiting an IC50 of 25 nM against human P2X3 homotrimers. This compound demonstrates significant anti-tussive activity without causing taste alterations. Camlipixant is primarily utilized in research focused on unexplained and refractory chronic cough. -
P2X7 Antagonist
JNJ-55308942 is a selective P2X7 antagonist with high affinity and significant brain penetration. It effectively inhibits the P2X7 receptor, demonstrating IC50 values of 10 nM for human and 15 nM for rat P2X7, along with corresponding Ki values of 7.1 nM and 2.9 nM. This compound is orally bioavailable and has been shown to block the release of IL-1β from adult rodent brain tissue, making it a valuable tool for investigating neuroinflammatory processes and related therapeutic applications. -
P2X1 Receptor Antagonist
NF023 hexasodium is a selective and competitive antagonist of the P2X1 receptor, demonstrating an IC50 value of 0.21 μM. While showing significantly higher IC50 values of 28.9 μM, > 50 μM, and > 100 μM for human P2X3, P2X2, and P2X4 receptor-mediated responses respectively, it provides a robust tool for investigating P2X1 receptor functions. This reagent is valuable in pharmacological research and studies exploring the role of purinergic signaling in various physiological and pathological processes. -
P2X4 Inhibitor
NP-1815-PX sodium is a selective inhibitor targeting the P2X4 receptor, exhibiting an IC50 of 0.26 μM against human P2X4 receptors. This compound effectively inhibits ATP-mediated prostaglandin production and attenuates TP receptor-induced calcium elevation, as well as NLRP3 inflammasome signaling. Notably, NP-1815-PX sodium demonstrates anti-allodynic effects in vivo and alleviates DNBS-induced colitis symptoms, including weight loss and tissue damage, through the downregulation of IL-1β levels and Caspase-1 activity. This reagent is applicable in research areas such as asthma and inflammatory bowel disease. -
P2X Receptor Antagonist
TNP-ATP triethylammonium is a selective antagonist of the P2X receptor, primarily involved in purinergic signaling. This compound exhibits significant antinociceptive effects in preclinical models, making it a valuable tool for investigating pain mechanisms. TNP-ATP triethylammonium can be utilized in research focused on pain modulation and the role of purinergic receptors in various physiological processes. -
P2X3 Antagonist
Eliapixant is a potent and selective antagonist of the P2X3 receptor, exhibiting an IC50 of 8 nM. It is primarily utilized in research related to refractory chronic cough, offering valuable insights into the mechanisms underlying this condition. The compound's specificity towards the P2X3 receptor makes it a valuable tool for studying purinergic signaling in respiratory pathways. -
P2X3 Receptor Antagonist
Sivopixant is a selective antagonist of the P2X3 receptor, exhibiting a potent inhibitory activity with an IC50 of 4.2 nM for P2X3 and 1100 nM for P2X2/3. This compound demonstrates significant analgesic properties, making it valuable for research focused on pain pathways and therapeutic applications in pain management. Sivopixant can be utilized in studies investigating the role of purinergic signaling in nociception and related disorders. -
P2X3 Antagonist
P2X3 antagonist 34 is a selective and orally active antagonist targeting the P2X3 homotrimeric receptor, demonstrating IC50 values of 25 nM, 92 nM, and 126 nM for human, rat, and guinea pig P2X3 receptors, respectively. This compound exhibits reduced activity against P2X2/3 heterotrimeric receptors, indicating a favorable selectivity profile. Its significant anti-tussive properties make P2X3 antagonist 34 a valuable tool for research in pain and respiratory conditions. -
P2X7 Receptor Antagonist
P2X7 receptor antagonist-2 is a selective antagonist of the P2X7 receptor, exhibiting a pIC50 value between 6.5 and 7.5. This compound demonstrates significant efficacy in reducing neuroinflammation, making it a valuable tool for research in neurodegenerative diseases and inflammatory conditions. Its ability to modulate P2X7 receptor activity positions it as a promising candidate for investigating therapeutic strategies targeting neuroinflammatory pathways. -
P2X3 Antagonist
Gefapixant citrate is a potent antagonist of the purinergic P2X3 receptor, exhibiting IC50 values of approximately 30 nM against recombinant human P2X3 homotrimers and 100-250 nM at human P2X2/3 heterotrimeric receptors. This compound is valuable for research related to chronic cough and knee osteoarthritis, providing insights into the modulation of nociceptive signaling pathways associated with these conditions. Its oral bioavailability further enhances its applicability in in vivo studies. -
P2X7 Receptor Antagonist
Lu AF27139 is a selective antagonist of the P2X7 receptor, exhibiting potent inhibitory activity with IC50 values of 12 nM and 2.4 nM for human and rat receptors, respectively. Additionally, it demonstrates effective inhibition in mouse, human, and rat models with Kis of 22, 54, and 13 nM. Due to its favorable pharmacokinetic profile, including oral activity and CNS penetration, Lu AF27139 is a valuable tool for investigating central nervous system diseases. -
P2X4 Receptor Inhibitor
Taspine is a natural product that functionally inhibits the P2X4 receptor, primarily through the inhibition of the PI3K signaling pathway. This compound exhibits notable anti-inflammatory activity by suppressing pro-inflammatory signaling in macrophages. Taspine is valuable for research applications focused on inflammation and immune responses, as well as studying the role of purinergic receptors in various pathological conditions. -
P2X7 Antagonist
JNJ-42253432 is a high-affinity orally active antagonist of the P2X7 receptor, exhibiting significant CNS penetration. With pKi values of 9.1 for rat and 7.9 for human P2X7 channels, it effectively modulates purinergic signaling. This compound is valuable for research on neuroinflammation, pain pathways, and other P2X7-related biological processes. -
P2X3 Receptor Antagonist
NF110 is a P2X3 receptor antagonist with a Ki of 36 nM, demonstrating selectivity as it is inactive toward stably expressed P2Y receptors (IC50s > 10 µM). It effectively inhibits alpha, beta-methylene-ATP-induced currents in rat dorsal root ganglia neurons, with an IC50 value of 527 nM. This compound is valuable for researching pain pathways and receptor signaling in nociceptive responses. -
P2-Receptor Agonist
2-Methylthio-ATP tetrasodium is a non-specific P2-receptor agonist that modulates purinergic signaling pathways. It has been shown to cause noncompetitive inhibition of ADP-induced aggregation in human platelets. This reagent is valuable for studies investigating platelet function, receptor signaling, and related cardiovascular research applications. -
P2X3 Receptor Antagonist
(E/Z)-Sivopixant is a selective antagonist of the P2X3 receptor, exhibiting an IC50 value of 4 nM. This compound demonstrates significant biological activity in modulating pain signals and neurogenic inflammation. It is primarily employed in research related to respiratory diseases, providing insights into potential therapeutic strategies for conditions associated with P2X3 receptor activation.
