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A 839977

Catalog No.GC15434

P2X7 antagonist,potent and selective

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A 839977 Chemical Structure

Cas No.: 870061-27-1

Size Price Stock Qty
10mg
$108.00
In stock
50mg
$399.00
In stock

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Sample solution is provided at 25 µL, 10mM.

Product Documents

Quality Control & SDS

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Background

A839977 is a novel and selective antagonist of P2X7 receptor with the IC50 values of 20 nM, 42nM and 150nM for human, rat and mouse, respectively [1].

A839977 has been reported to block BzATP-evoked changes in intracellular calcium concentrations in 132N1 cells stable expressing P2X7 receptors with the IC50 values of 20 nM, 42nM and 150nM for human, rat and mouse, respectively. In addition, A839977 has also revealed to inhibit BzATP-stimulated IL-1β release and YO-PRO uptake with the IC50 of 37nM and 7nM, respectively, in differentiated human THP-1 cells. Besides, A839977 has been noted to produce parallel rightward shifts in BzATP concentration-effect calcium influx curves with the pAα value of 8.1. Apart from these, A839977 has been exhibited to reduce CFA-induced thermal hyperalgesia in a dose-dependent fashion with the ED50 value of 100μmol/kg(i.p.) [1].

References:
[1] Honore P1, Donnelly-Roberts D, Namovic M, Zhong C, Wade C, Chandran P, Zhu C, Carroll W, Perez-Medrano A, Iwakura Y, Jarvis MF. The antihyperalgesic activity of a selective P2X7 receptor antagonist, A-839977, is lost in IL-1alphabeta knockout mice. Behav Brain Res. 2009 Dec 1;204(1):77-81.

Chemical Properties

Cas No. 870061-27-1 SDF
Chemical Name (E)-N-(1-(2,3-dichlorophenyl)-1H-tetrazol-5(2H)-ylidene)-1-(2-(pyridin-2-yloxy)phenyl)methanamine
Canonical SMILES ClC1=C(Cl)C(N2/C(N=NN2)=N\CC3=CC=CC=C3OC4=CC=CC=N4)=CC=C1
Formula C19H14Cl2N6O M.Wt 413.26
Solubility Soluble in DMSO 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 2.4198 mL 12.0989 mL 24.1978 mL
5 mM 0.484 mL 2.4198 mL 4.8396 mL
10 mM 0.242 mL 1.2099 mL 2.4198 mL
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Average Rating: 5 ★★★★★ (Based on Reviews and 4 reference(s) in Google Scholar.)

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