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A 839977

Catalog No.
B1282
P2X7 antagonist,potent and selective
Grouped product items
SizePriceStock Qty
10mg
$207.00
Ship with 10-15 days
50mg
$845.00
Ship with 10-15 days

Tel: +1-832-696-8203

Email: [email protected]

Worldwide Distributors

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

Physical AppearanceWhite solid
StorageStore at -20°C
M.Wt413.26
Cas No.870061-27-1
FormulaC19H14Cl2N6O
SolubilitySoluble in DMSO
Chemical Name(E)-N-(1-(2,3-dichlorophenyl)-1H-tetrazol-5(2H)-ylidene)-1-(2-(pyridin-2-yloxy)phenyl)methanamine
SDFDownload SDF
Canonical SMILESClC1=C(Cl)C(N2/C(N=NN2)=N\CC3=CC=CC=C3OC4=CC=CC=N4)=CC=C1
Shipping ConditionShip with blue ice, or upon other requests.
General tipsFor obtaining a higher solubility, please warm the tube at 37°C and shake it in the ultrasonic bath for a while. We do not recommend long-term storage for the solution, please use it up soon.

Quality Control

Quality Control & MSDS

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Chemical structure

A 839977