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AZ 11645373

Catalog No.
B7362
Human P2X7 antagonist,potent and selective
Grouped product items
SizePriceStock Qty
10mg
$299.00
Ship with 5-10 days
50mg
$1,229.00
Ship with 5-10 days

Tel: +1-832-696-8203

Email: [email protected]

Worldwide Distributors

Background

AZ11645373 is identified as a highly selective and potent antagonist of human P2X7 receptors but not mouse/rat P2X7 receptors.

Adenosine 5′-triphosphate (ATP)-gated P2X receptors (P2XRs) comprise of seven genes which encode plasma membrane ion channels for calcium cation. These proteins are differentially expressed throughout autonomic, sensory and central neurons as well as in visceral smooth muscle, epithelia and immune cells. P2XRs was also reported to have potential roles in acute and/or chronic pain sensation.

In cellular culture, treatment of AZ11645373 inhibited human P2X7 receptor responses in HEK cells, which dislayed in a non-surmountable manner with K B values ranging from 5 - 20 nM 1. K B values were not altered by removing extracellular calcium and magnesium. In addition, AZ11645373 treatment inhibited ATP-evoked IL-1β release from lipopolysaccharide- activated THP-1 cells with IC50 = 90 nM 1.

Regarding the effect of AZ11645373 administration in vivo, the evidence should be provided by performing the study in human or mice or other animal models.

Reference:
1.  Stokes L, Jiang LH, Alcaraz L, et al. Characterization of a selective and potent antagonist of human P2X(7) receptors, AZ11645373. British journal of pharmacology. 2006;149(7):880-887.

Chemical Properties

Physical AppearanceOff White solid
StorageStore at -20°C
M.Wt463.51
Cas No.227088-94-0
FormulaC24H21N3O5S
Solubilityinsoluble in DMSO
Chemical Name(R)-3-(1-((3'-nitro-[1,1'-biphenyl]-4-yl)oxy)-4-(pyridin-4-yl)butan-2-yl)thiazolidine-2,4-dione
SDFDownload SDF
Canonical SMILESO=C1N(C(SC1)=O)[[email protected]@H](COC2=CC=C(C3=CC=CC([N+]([O-])=O)=C3)C=C2)CCC4=CC=NC=C4
Shipping ConditionEvaluation sample solution : ship with blue ice.All other available size: ship with RT , or blue ice upon request
General tipsFor obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months.

Quality Control

Quality Control & MSDS

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Chemical structure

AZ 11645373