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CAS No. : 870061-27-1
MCE 国际站:A 839977
产品活性:A 839977是一种选择性 P2X7 受体拮抗剂, 可阻断人和大小鼠 P2X7 受体的 BzATP 诱发的钙内流 (IC50s=20 nM, 42 nM / 150 nM); 在体实验中, 通过阻断 IL-1β 释放产生抗痛觉过敏反应, 减弱模型动物的炎症反应与神经性疼痛.
研究领域:Membrane Transporter/Ion Channel
作用靶点:P2X Receptor
In Vitro: A 839977 selectively blocks BzATP-evoked calcium influx at mammalian P2X7 receptors, (IC50=20-150 nM), which blocks agonist-evoked YO-PRO uptake and IL-1beta release from differentiated human THP-1 cells, it has been shown to reduce inflammatory and neuropathic pain in animal models.A 839977 (50 nM, pre-treatment 1 hour) significantly prevents pressure-induced rise of IL-1β priming in optic nerve astrocytes.
In Vivo: A 839977 (30 μmol/kg, 100 μmol/kg, 300 μmol/kg; pre-injected 30mins) dose-dependently reduces thermal hyperalgesia produced by intraplantar administration of complete Freund's adjuvant (CFA) in rats.
A 839977 (10 μmol/kg, 30 μmol/kg, 100 μmol/kg; pre-injected 30mins) produces robust antihyperalgesia in the CFA model of inflammatory pain in wild-type mice, but it has no effect on IL-1alphabeta knockout mice.
A 839977 attenuates dorsal horn neuronal responses in cancer bearing animals.
相关产品:Bioactive Compound Library Plus | Immunology/Inflammation Compound Library | Membrane Transporter/Ion Channel Compound Library | Pyroptosis Compound Library | Neurotransmitter Receptor Compound Library | Targeted Diversity Library | Heterocyclic Compound Library | Membrane Protein-targeted Compound Library | Membrane Receptor-targeted Compound Library | Highly Selective Inhibitors Library | (E/Z)-Sivopixant | AF-353 | Gefapixant | P2X3 antagonist 34 | Minodronic acid | MRS4738 | AZ 11645373 | Indophagolin | PPNDS tetrasodium | Bullatine A | JNJ-54166060 | P2X7 receptor antagonist-2 | A-317491 | Ro-51 | A-804598 | P2X7-IN-2 TFA | α,β-Methylene-ATP | A 438079 hydrochloride | Taspine | Blue FPG-A trisodium | GSK-1482160 | KN-62 | JNJ-55308942 | Zeaxanthin dipalmitate | H-Lys-Tyr-OH TFA | Lu AF27139 | GW791343 dihydrochloride | NF279 | JNJ-54175446
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