A-839977 | B2973

A-839977 is a potent antagonist of the purinergic receptor P2X subtype 7 (P2X7). A-839977 potently blocks BzATP-induced calcium influx at recombinant human, rat and mouse P2X7 receptors with IC₅₀ values of 20 nM, 42 nM and 150 nM respectively. It also potently blocks agonist-induced YO-PRO uptake and IL-1β release from differentiated human THP-1 cells. It shows antihyperalgesic and antinociceptive effects in animal models of inflammatory pain.

A-839977 is a potent antagonist of the purinergic receptor P2X subtype 7 (P2X7). A-839977 potently blocks BzATP-induced calcium influx at recombinant human, rat and mouse P2X7 receptors with IC₅₀ values of 20 nM, 42 nM and 150 nM respectively. It also potently blocks agonist-induced YO-PRO uptake and IL-1β release from differentiated human THP-1 cells. It shows antihyperalgesic and antinociceptive effects in animal models of inflammatory pain.

B2973 | A-839977 DataSheet

Alternate Name/Synonyms: 1-(2,3-dichlorophenyl)-N-[(2-pyridin-2-yloxyphenyl)methyl]tetrazol-5-amine

Appearance: Solid

Formulation:

CAS Number: 870061-27-1

Structure Available?: True

Peptide sequence:

Salt Form: false

Molecular Formula: C₁₉H₁₄Cl₂N₆O

Molecular Weight: 413.26

Cell-Permeable?: True

Purity: 98%

Solubilities: Soluble in DMSO in 0

Handling: Do not take internally. Wear gloves and mask when handling the product! Avoid contact by all modes of exposure.

Country of Origin: USA

Tag Line: A potent P2X7 antagonist

MDL Number: MFCD19690959

PubChem CID: 53325875

SMILES: C1=CC=C(C(=C1)CNC2=NN=NN2C3=C(C(=CC=C3)Cl)Cl)OC4=CC=CC=N4

InChi: InChI=1S/C19H14Cl2N6O/c20-14-7-5-8-15(18(14)21)27-19(24-25-26-27)23-12-13-6-1-2-9-16(13)28-17-10-3-4-11-22-17/h1-11H,12H2,(H,23,24,26)

InChi Key: GMVNBKZQJFRFAR-UHFFFAOYSA-N