A 804598 |
| カタログ番号GC17870 |
A 804598 は、マウス、ラット、およびヒトの P2X7 受容体に対する IC50 がそれぞれ 9 nM、10 nM、および 11 nM である、CNS 浸透性、競合的および選択的な P2X7 受容体アンタゴニストです。
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 1125758-85-1
Sample solution is provided at 25 µL, 10mM.
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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.
| 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 |
| 溶解度 | 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. | ||
| Prepare stock solution | |||
|
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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Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
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Quality Control & SDS
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- Purity: >98.50%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
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Average Rating: 5 (Based on Reviews and 39 reference(s) in Google Scholar.)
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