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A 804598
本产品不向个人销售，仅用作科学研究，不用于任何人体实验及非科研性质的动物实验。
A 804598图片
CAS NO:1125758-85-1
包装与价格：
包装价格(元)
10mg电议
50mg电议

产品介绍
A 804598 是一种 CNS 渗透性、竞争性和选择性 P2X7 受体拮抗剂，对小鼠、大鼠和人 P2X7 受体的 IC50 分别为 9 nM、10 nM 和 11 nM。
Cas No.1125758-85-1
Canonical SMILESN#CN/C(NC1=C2C(N=CC=C2)=CC=C1)=N\[C@@H](C)C3=CC=CC=C3
分子式C19H17N5
分子量315.37
溶解度DMF: 30 mg/ml,DMSO: 30 mg/ml,DMSO:PBS (pH 7.2) (1:20): 0.05 mg/ml
储存条件Store at -20°C
General tipsFor obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.
Shipping ConditionEvaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request
产品描述

A 804598 is a potent and selective antagonist of P2X7 receptor with IC50 values of 8.9, 9.9 and 10.9 nM for mouse, rat and human P2X7 receptors, respectively [1].

P2X purinoceptor 7 (P2X7 receptor) is a purinoceptor and is activated by high concentrations of ATP. P2X7 receptor plays an important role in ATP-mediated cell death, inflammation and regulation of receptor trafficking.

A 804598 is a potent and selective P2X7 receptor antagonist. In differentiated THP-1 cells that expressed human P2X7 receptors, A 804598 inhibited BzATP stimulated Yo-Pro uptake and release of IL-1β. In 1321N1 cells expressed recombinant rat P2X7 receptor, A 804598 showed high affinity with Kd = 2.4 nM [1]. A 804598 inhibited BZ-ATP stimulated calcium influx with IC50 value of 28.71 nM in a concentration-dependent way. A-804598 was a potent P2X7 receptor antagonist with Ki value of 7.51 nM [2].

In adult male rats, footshock increased the mRNA levels of CD14 and IL-1β in the paraventricular nucleus. While A-804598 (25 mg/kg) partially inhibited these effects [3].

References:
[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.