human p2x7 receptor

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.

Oxatomide (Oxatomida) is a potent and orally active dual H1 histamine receptor and P2X7 receptor antagonist with antihistamine and antiallergic activity.Oxatomide can be used to block ATP-induced currents in the human P2X7 receptor with an IC50 value of 0.95 μM.Oxatomide has an inhibitory effect on ATP-induced Ca2+ inward currents with an IC50 value of 0.43 μM.Oxatomide inhibits 5-hydroxytryptamine. Oxatomide inhibits 5-hydroxytryptamine with an IC50 of 0.43 μM.Oxatomide is used in the treatment of immune system diseases and in the study of hypersensitivity reactions.

5-(N,N-Hexamethylene)-amiloride (5-HMA) is an amiloride derivative that inhibits TRPA1-mediated calcium signaling (IC50: 35 μM). It functions as an inhibitor of the Na+ H+ exchanger (NHE) with Ki values ranging from 0.013 to 2.4 μM for various NHE isoforms. Additionally, 5-HMA blocks ASIC3 channels by 51% at 20 μM.

Tanshinone IIA sulfonate sodium (Tanshinone IIA sodium sulfonate) is a water-soluble derivative of tanshinone IIA extracted from Savia miltiorrhiza; a potent negative allosteric modulator of the human purinergic receptor P2X7. Tanshinone IIA sulfonate sodium (12.5 μM) inhibits hypoxia-induced PKG and PPAR-γ downregulation in PASMCs and distal pulmonary arteries of rats.

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

A-740003 (A 740003) is an effective and specific P2X7 receptor antagonist (IC50: 18 40 nM, for rat human). It can reduce nociception in animal models of persistent neuropathic and inflammatory pain, and also reduce neuroblastoma tumor growth in mice.

AZ 11645373 (3-[1-[[(3'-NITRO[1,1'-BIPHENYL]-4-YL)OXY]METHYL]-3-(4-PYRIDINYL)PROPYL]-2,4-THIAZOLIDINEDIONE) is a highly selective and potent human P2X7 receptor antagonist that has no effect on mouse rat P2X7 receptor.

JNJ-47965567 (JNJ-479655) is a selective antagonist of the purinergic receptor P2X subtype 7 (P2X7), a ligand-gated ion channel(with pKis of 7.9 and 8.7 for human and rat P2X7, respectively).

BAY-1797 is an orally active and selective P2X4 antagonist (IC50: 211 nM against human P2X4) with anti-nociceptive and anti-inflammatory effects. BAY-1797 displays no or very weak activity on the other P2X ion channels.

A-839977 is a selective P2X7 receptor antagonist with anti-inflammatory and analgesic properties, inhibiting BzATP-induced calcium efflux from the P2X7 receptor, and is used in the study of renal fibrosis.

JNJ-54166060 is a potent and selective P2X7 receptor antagonist, with IC50 values of 4 nM, 115 nM, and 72 nM for the human, rat, and mouse P2X7 receptors, respectively [1].

ITH15004 is a non-nucleotide antagonist of the purinergic P2X7receptor (IC50= 9 μM in HEK293 cells expressing the human receptor).1It inhibits ATP-induced currents inX. laevisoocytes expressing the human P2X7receptor when used at a concentration of 100 μM. ITH15004 (1 μM) decreases IL-1β release from LPS-primed, ATP-stimulated isolated mouse peritoneal macrophages. It has high permeability in a parallel artificial membrane permeability assay (PAMPA). 1.Calzaferri, F., Narros-Fernández, P., de Pascual, R., et al.Synthesis and pharmacological evaluation of novel non-nucleotide purine derivatives as P2X7 antagonists for the treatment of neuroinflammationJ. Med. Chem.64(4)2272-2290(2021)

GW791343 trihydrochloride (GW791343 3HCl) is aHCl salt form of GW791343, which is a non-competitive allosteric modulator of human P2X7 receptor inhibitor with pIC50 of 7.

P2X7 receptor antagonist-3 is a potent inhibitor of the P2X7 receptor, with IC50 values of 4.2 nM in humans and 6.8 nM in rats, demonstrating its high efficacy across species.

CI 75300 targets the P2X purinoceptor 7 (human).

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.