Seven cation permeable ligand-gated ion channels (LGICs) known as P2X receptors (P2X1R-P2X7R) are a family of LGICs that open in response to the extracellular ligand adenosine 5′-triphosphate (ATP) binding. P2X receptors are widely expressed in the nervous, immune, cardiovascular, skeletal, gastrointestinal, respiratory, and endocrine systems and have a high permeability to Ca2+, Na+, and K+.
P2X receptors are extensively expressed in both excitatory and non-excitatory cells, including neuron, glia, platelet, epithelia, and macrophages. They play a key role in a number of critical physiological and pathological processes, such as synaptic transmission, pain perception, inflammation, cardiovascular regulation, immune modulation, and tumorigenesis.
| Structure | Cat No. | Product Name | CAS No. | Product Description |
|---|---|---|---|---|
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V73562 | (E/Z)-Sivopixant ((E/Z)-S-600918) | 1640808-39-4 | (E/Z)-Sivopixant ((E/Z)-S-600918) is a potent P2X3 receptor antagonist (inhibitor) with IC50 of 4 nM. |
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V73572 | 8-Bromo-ATP (8-Bromoadenosine 5'-triphosphate; 8-Br-ATP) | 23567-97-7 | 8-Bromo-ATP (8-Bromoadenosine 5'-triphosphate), an ATP analog, is an agonist of the purinergic P2X receptor. |
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V28878 | A 438079 | 899507-36-9 | A-438079 HCl is a novel, potent, and selective P2X7 receptor antagonist with pIC50 of 6.9. |
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V2791 | A-317491 | 475205-49-3 | A-317491 is a selective non-nucleotide antagonist of P2X3 and P2X2/3 receptors, which inhibits calcium flux mediated by the receptors. |
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V3090 | A-317491 Sodium | 475205-49-3 | A-317491 sodium, the tri-sodium salt of A-317491, which is a selective non-nucleotide antagonist of P2X3 and P2X2/3 receptors, which inhibits calcium flux mediated by the receptors. |
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V4252 | AZD9056 hydrochloride | 345303-91-5 | AZD9056 hydrochloride is a novel, potent, selective, orally bioavailable antagonist of P2X7 receptor which is an adenosine triphosphate (ATP)-gated cation channel expressed on a variety of cell types believed to play a role in inflammation. |
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V77178 | BzATP triethylammonium salt | BzATP triethylammonium salt is a P2X receptor agonist/activator with pEC50s of 8.74, 5.26, 7.10, 7.50, 6.19, 6.31 and 5.33 for P2X1, P2X2, P2X3, P2X2/3, P2X4 and P2X7 respectively. | |
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V73561 | Camlipixant (BLU-5937) | 1621164-74-6 | Camlipixant (BLU-5937) is a specific, noncompetitive and orally bioactive P2X3 homotrimer receptor antagonist (inhibitor) with IC50 of 25 nM for hP2X3 homotrimer. |
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V77029 | EVT-401 | EVT-401 (P2X7 receptor blocker (antagonist)-1) is a purinergic P2X7 receptor blocker (antagonist). | |
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V73563 | Filapixant (BAY 1902607) | 1948232-63-0 | Filapixant is a purinergic receptor antagonist. |
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V2116 | Gefapixant (AF219; MK-7264) | 1015787-98-0 | Gefapixant (also known as AF-219 and MK-7264) is a novel, potent, and orally bioactive P2X3 receptor (P2X3R) antagonist with antitussive effects, and may be used forchronic cough. |
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V4926 | GW791343 trihydrochloride | 1019779-04-4 | GW-791343 3HCl, thetrihydrochloride salt form ofGW-791343 (GW791343) is a novel, potent P2X7 allosteric modulator that exhibits species-specific activity and acts as a negative allosteric modulator of human P2X7 with pIC50 of 6.9 - 7.2. |
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V73582 | GW791343 trihydrochloride | 309712-55-8 | GW791343 tri HCl is a potent NAM (negative allosteric modulator) (species-specific) of human P2X7 receptor, which produces noncompetitive antagonism to human P2X7 receptor, with pIC50 of 6.9-7.2. |
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V80047 | H-Lys-Tyr-OH TFA (Lysyltyrosine TFA) | H-Lys-Tyr-OH TFA (Lysyltyrosine TFA) is a dipeptide consisting of L-lysine and L-tyrosine. | |
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V2339 | Indophagolin | 1207660-00-1 | Indophagolin is a potent indoline-containing autophagy inhibitor (IC50=140 nM). |
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V73581 | Iso-PPADS tetrasodium | 207572-67-6 | Iso-PPADS tetrasodium is a P2X-purinoceptor receptor antagonist. |
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V85134 | ITH15004 | 2600675-12-3 | |
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V73578 | JNJ-54166060 | 1627900-41-7 | JNJ-54166060 is a P2X7 receptor blocker (antagonist), with IC50s of 4/115/72 nM for human/rat/mouse P2X7 receptors respectively. |
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V73559 | JNJ-55308942 | 2166558-11-6 | JNJ-55308942 is a high-affinity, selective, BBB (blood-brain barrier) permeable (penetrable) P2X7 functional antagonist (hP2X7: IC50=10 nM, Ki=7.1 nM; rP2X7: IC50=15 nM, Ki=2.9 nM). |
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V2508 | Lu AF27139 | 2097117-06-9 | Lu AF27139a novel rodent-active and CNS-penetrant P2X7 receptor antagonist, which is highly selective and potent against rat, mouse, and human forms of the receptors. |
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