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Submit ReviewA 804598
说明： Potent and selective P2X7 antagonist
化学名： N-Cyano-N"-[(1S)-1-phenylethyl]-N'-5-quinolinyl-guanidine
纯度： ≥99% (HPLC)
生物活性 for A 804598
A 804598 is a potent, competitive P2X7 receptor antagonist (IC50 values are 8.9, 9.9 and 10.9 nM for mouse, rat and human P2X7 receptors respectively). Selective for P2X7 receptors (IC50 > 5-10 μM for a wide array of cell surface receptors and ion channels). Binds with high affinity (Ki app = 2.4 nM for rat P2X7 receptors).
化合物库 for A 804598
A 804598 is also offered as part of the Tocriscreen 2.0 Max. 了解 Tocris 化合物库的更多信息。
技术数据 for A 804598
| 分子量 | 315.37 |
| 公式 | C19H17N5 |
| 储存 | Store at -20°C |
| 纯度 | ≥99% (HPLC) |
| CAS Number | 1125758-85-1 |
| PubChem ID | 53325874 |
| InChI Key | PQYCRDPLPKGSME-AWEZNQCLSA-N |
| Smiles | C[C@@H](C3=CC=CC=C3)NC(NC2=CC=CC1=NC=CC=C12)=NC#N |
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.
溶解性数据 for A 804598
| 溶剂 | 最高浓度 mg/mL | 最高浓度 mM | |
|---|---|---|---|
| 溶解性 | |||
| DMSO | 31.54 | 100 |
制备储备液 for A 804598
以下数据基于产品分子量 315.37。 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
| 浓度/溶剂体积/质量 | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 1 mM | 3.17 mL | 15.85 mL | 31.71 mL |
| 5 mM | 0.63 mL | 3.17 mL | 6.34 mL |
| 10 mM | 0.32 mL | 1.59 mL | 3.17 mL |
| 50 mM | 0.06 mL | 0.32 mL | 0.63 mL |
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产品说明书 for A 804598
参考文献 for A 804598
参考文献是支持产品生物活性的出版物。
Donnelly-Roberts et al (2009) [3H]A-804598 ([3H]2-cyano-1-[(1S)-1-phenylethyl]-3-quinolin-5-ylguanidine) is a novel, potent, and selective antagonist radioligand for P2X7 receptors. Neuropharmacology 56 223 PMID: 18602931
Able et al (2011) Receptor localization, native tissue binding and ex vivo occupancy for centrally penetrant P2X7 antagonists in the rat. Br.J.Pharmacol. 162 405 PMID: 20840537
If you know of a relevant reference for A 804598, please let us know.
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关键词: A 804598, A 804598 supplier, A804598, purinergic, receptors, P2X7, antagonists, inhibitors, inhibits, potent, selective, competitive, high, affinity, P2X, Receptors, 4473, Tocris Bioscience
3 篇 A 804598 的引用文献
引用文献是使用了 Tocris 产品的出版物。 A 804598 的部分引用包括：
Dosch et al (2019) Connexin-43-dependent ATP release mediates macrophage activation during sepsis. Elife 8 PMID: 30735126
Young et al (2015) A novel mechanism of autophagic cell death in dystrophic muscle regulated by P2RX7 receptor large-pore formation and HSP90. Cell Commun Signal 11 113 PMID: 25700737
Yuri et al (2022) Blocking of P2X7r Reduces Mitochondrial Stress Induced by Alcohol and Electronic Cigarette Exposure in Brain Microvascular Endothelial Cells. Antioxidants (Basel) 11 PMID: 35883819
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A 804598 的评论
平均评分: 5 (Based on 1 Review.)
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A 804598 inhibits LPS-induced inflammation.
By
Anonymous on 01/22/2019
分析类型： In Vitro
种属： Mouse
细胞系/组织： Macrophages
RAW macrophages were stimulated with LPS (200 ng/ml) in the absence or presence of A 804598 (1 μM) or MRS 2578 (100 μM) for 8 h to follow iNOS expression by qPCR. Both compounds inhibited LPS-induced iNOS expression revealing role of purinergic receptors.
该领域的文献
Tocris offers the following scientific literature in this area to showcase our products. We invite you to request* your copy today!
*请注意，Tocris 仅会向正规科研企业/机构地址发送文献。
P2X and P2Y Receptors Scientific Review
Written by Kenneth Jacobson, this review provides an overview of the different subtypes and structures of the P2 receptor families, as well as the pharmacological probes used to study them; compounds available from Tocris are listed.