A 804598
mRNA synthesis
In vitro transcription of capped mRNA with modified nucleotides and Poly(A) tail
Tyramide Signal Amplification (TSA)
TSA (Tyramide Signal Amplification), used for signal amplification of ISH, IHC and IC etc.
Phos Binding Reagent Acrylamide
Separation of phosphorylated and non-phosphorylated proteins without phospho-specific antibody
Cell Counting Kit-8 (CCK-8)
A convenient and sensitive way for cell proliferation assay and cytotoxicity assay
SYBR Safe DNA Gel Stain
Safe and sensitive stain for visualization of DNA or RNA in agarose or acrylamide gels.
Inhibitor Cocktails
Protect the integrity of proteins from multiple proteases and phosphatases for different applications.
A 804598是P2X7受体的强效选择性拮抗剂，对小鼠、大鼠和人P2X7受体的IC50值分别为8.9、9.9和10.9 nM[1]。
P2X嘌呤受体7（P2X7受体）是一种嘌呤受体，由高浓度的三磷酸腺苷激活。P2X7受体在ATP介导的细胞死亡、炎症和受体转运调节中起重要作用。
A 804598是P2X7受体的强效选择性拮抗剂。在表达人P2X7受体的分化THP-1细胞中，A 804598抑制BzATP刺激的Yo-Pro摄取和IL-1β的释放。在表达重组大鼠P2X7受体的1321N1细胞中，A 804598表现出高亲和力，Kd值为2.4 nM[1]。A 804598以浓度依赖性的方式抑制BZ-ATP诱导的钙离子内流，IC50值为28.71 nM。A 804598是P2X7受体的强效拮抗剂，Ki值为7.51 nM [2]。
在成年雄性大鼠中，电击室旁核增加CD14和IL-1β的mRNA水平。而25 mg/kg的A-804598可部分抑制这些效果[3]。
参考文献：
[1]. Donnelly-Roberts DL, Namovic MT, Surber B, et al. [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, 2009, 56(1): 223-229.?
[2]. Able SL, Fish RL, Bye H, et al. Receptor localization, native tissue binding and ex vivo occupancy for centrally penetrant P2X7 antagonists in the rat. Br J Pharmacol. 2011, 162(2): 405-414.
[3]. Catanzaro JM1, Hueston CM, Deak MM, et al. The impact of the P2X7 receptor antagonist A-804598 on neuroimmune and behavioral consequences of stress. Behav Pharmacol, 2014, 25(5-6): 582-598.
| Physical Appearance | A crystalline solid |
| Storage | Store at -20°C |
| M.Wt | 315.37 |
| Cas No. | 1125758-85-1 |
| Formula | C19H17N5 |
| Solubility | insoluble in EtOH; insoluble in H2O; ≥47 mg/mL in DMSO |
| SDF | Download SDF |
| Canonical SMILES | N#CN/C(NC1=C2C(N=CC=C2)=CC=C1)=N\[C@@H](C)C3=CC=CC=C3 |
| 运输条件 | 蓝冰运输或根据您的需求运输。 |
| 一般建议 | 不同厂家不同批次产品溶解度各有差异，仅做参考。若实验所需浓度过大至产品溶解极限，请添加助溶剂助溶或自行调整浓度。溶液形式一般不宜长期储存，请尽快用完。 |
质量控制和MSDS
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化学结构
