Description
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.
Product information
CAS Number: 227088-94-0
Molecular Weight: 463.51
Formula: C24H21N3O5S
Chemical Name: 3-[(2R)-1-({3'-nitro-[1,1'-biphenyl]-4-yl}oxy)-4-(pyridin-4-yl)butan-2-yl]-1,3-thiazolidine-2,4-dione
Smiles: [O-][N+](=O)C1=CC(=CC=C1)C1C=CC(=CC=1)OC[C@@H](CCC1C=CN=CC=1)N1C(=O)SCC1=O
InChiKey: VQEHBLGYANQWEA-OAQYLSRUSA-N
InChi: InChI=1S/C24H21N3O5S/c28-23-16-33-24(29)26(23)21(7-4-17-10-12-25-13-11-17)15-32-22-8-5-18(6-9-22)19-2-1-3-20(14-19)27(30)31/h1-3,5-6,8-14,21H,4,7,15-16H2/t21-/m1/s1
Technical Data
Appearance: Solid Power
Purity: ≥98% (or refer to the Certificate of Analysis)
Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis
Storage Condition: Dry, dark and -20 oC for 1 year or refer to the Certificate of Analysis.
Shelf Life: ≥12 months if stored properly.
Stock Solution Storage: 0 - 4 oC for 1 month or refer to the Certificate of Analysis.
Drug Formulation: To be determined
HS Tariff Code: 382200
Products are for research use only. Not for human use.
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