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Submit ReviewA 839977 is a potent P2X7 antagonist; blocks BzATP-evoked calcium influx at recombinant human, rat and mouse P2X7 receptors (IC50 values are 20, 42 and 150 nM respectively). Displays antinociceptive effects in rat and mice models of inflammatory pain. CNS penetrant.
分子量 | 413.26 |
公式 | C19H14Cl2N6O |
储存 | Store at +4°C |
纯度 | ≥98% (HPLC) |
CAS Number | 870061-27-1 |
PubChem ID | 53325875 |
InChI Key | GMVNBKZQJFRFAR-UHFFFAOYSA-N |
Smiles | ClC(C(Cl)=CC=C4)=C4N1N=NN=C1NCC2=CC=CC=C2OC3=NC=CC=C3 |
上方提供的技术数据仅供参考。批次相关数据请参见分析证书。
Tocris products are intended for laboratory research use only, unless stated otherwise.
参考文献是支持产品生物活性的出版物。
Honore et al (2009) The antihyperalgesic activity of a selective P2X7 receptor antagonist, A-839977, is lost in IL-1αβ knockout mice. Behav.Brain.Res. 204 77 PMID: 19464323
Friedle et al (2010) Recent patents on novel P2X7 receptor antagonists and their potential for reducing central nervous system inflammation. Recent Pat.CNS Drug Discov. 5 35 PMID: 19705995
关键词: A 839977, A 839977 supplier, A839977, purinergics, purinoceptors, purines, p2x7, antagonists, antinociceptive, cns, penetrant, P2X, Receptors, 4232, Tocris Bioscience
引用文献是使用了 Tocris 产品的出版物。 A 839977 的部分引用包括:
Gangadharan et al (2015) Caveolin-1 regulates P2X7 receptor signaling in osteoblasts. PLoS One 308 C41 PMID: 25318104
Wennan et al (2020) Polarized Cytokine Release Triggered by P2X7 Receptor from Retinal Pigmented Epithelial Cells Dependent on Calcium Influx. Cells 9 PMID: 33255431
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