A P2X7 receptor antagonist; inhibits BzATP-evoked intracellular calcium influx in 1321N1 cells expressing human

A-839977 – 1 mg

Brand:
Cayman
CAS:
870061-27-1
Storage:
-20
UN-No:
Non-Hazardous - /

A-389977 is an antagonist of the purinergic P2X7 receptor.{57152} It inhibits BzATP-evoked intracellular calcium influx in 1321N1 cells expressing human, rat, and mouse receptors (IC50s = 20, 42, and 150 nM, respectively). A-839977 inhibits BzATP-induced YO-PRO dye uptake, a marker of membrane pore formation, and IL-1β release from THP-1 cells (IC50s = 6.6 and 37 nM, respectively). In vivo, A-389977 (30, 100, and 300 µmol/kg, i.p.) reduces thermal hyperalgesia in rats. A-389977 (40 mg/kg) reduces thermal and mechanical hyperalgesia in a rat MRMT-1 mammary carcinoma model of cancer-induced bone pain.{57151}  

 

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SKU: 30934 - 1 mg Category:

Description

A P2X7 receptor antagonist; inhibits BzATP-evoked intracellular calcium influx in 1321N1 cells expressing human, rat, and mouse receptors (IC50s = 20, 42, and 150 nM, respectively); inhibits BzATP-induced YO-PRO dye uptake and IL-1β release from THP-1 cells (IC50s = 6.6 and 37 nM, respectively); reduces thermal hyperalgesia in rats at 30, 100, and 300 µmol/kg, i.p.; reduces thermal and mechanical hyperalgesia in a rat MRMT-1 mammary carcinoma model of cancer-induced bone pain at 40 mg/kg

Formal name: 1-(2,3-dichlorophenyl)-N-[[2-(2-pyridinyloxy)phenyl]methyl]-1H-tetrazol-5-amine

Synonyms: 

Molecular weight: 413.3

CAS: 870061-27-1

Purity: ≥98%

Formulation: A crystalline solid

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