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A 804598

Catalog No.GC17870

A 804598 est un antagoniste des récepteurs P2X7, compétitif et sélectif, pénétrant dans le SNC, avec des IC50 de 9 nM, 10 nM et 11 nM pour les récepteurs P2X7 de la souris, du rat et de l'homme, respectivement.

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A 804598 Chemical Structure

Cas No.: 1125758-85-1

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10mg
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50mg
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Sample solution is provided at 25 µL, 10mM.

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Background

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.

Chemical Properties

Cas No. 1125758-85-1 SDF
Canonical SMILES N#CN/C(NC1=C2C(N=CC=C2)=CC=C1)=N\[C@@H](C)C3=CC=CC=C3
Formula C19H17N5 M.Wt 315.37
Solubility DMF: 30 mg/ml,DMSO: 30 mg/ml,DMSO:PBS (pH 7.2) (1:20): 0.05 mg/ml Storage Store at -20°C
General tips Please select the appropriate solvent to prepare the stock solution according to the solubility of the product in different solvents; once the solution is prepared, please store it in separate packages to avoid product failure caused by repeated freezing and thawing.Storage method and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored at -20°C, please use it within 1 month.
To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time.
Shipping Condition Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request.

Complete Stock Solution Preparation Table

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1 mg 5 mg 10 mg
1 mM 3.1709 mL 15.8544 mL 31.7088 mL
5 mM 0.6342 mL 3.1709 mL 6.3418 mL
10 mM 0.3171 mL 1.5854 mL 3.1709 mL
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Average Rating: 5 ★★★★★ (Based on Reviews and 39 reference(s) in Google Scholar.)

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