A 839977

SKU: orb1707735

Description

A 839977

Research Area

Metabolism Research, Neuroscience, Pharmacology & Drug Discovery

Key Properties

• CAS Number: 870061-27-1
• MW: 413.26
• Purity: 98.01%
• Formula: C₁₉H₁₄Cl₂N₆O
• SMILES: Clc1cccc(c1Cl)-n1nnnc1NCc1ccccc1Oc1ccccn1
• Target: P2X Receptor,Calcium Channel
• Solubility: DMSO:80 mg/mL (193.58 mM);10% DMSO+40% PEG300+5% Tween 80+45% Saline:3.3 mg/mL (7.99 mM)

Bioactivity

• Target IC50:
  P2X7 receptor:150 nM (Mouse)|P2X7 receptor:42 nM (Rat)|P2X7 receptor:20 nM (Human)
• In Vivo:
  In rats, A 839977 (30 μmol/kg, 100 μmol/kg, 300 μmol/kg; pre-injected 30 mins) dose-dependently reduces thermal hyperalgesia induced by intraplantar administration of complete Freund's adjuvant (CFA).In the CFA model of inflammatory pain in wild-type mice, A 839977 (10 μmol/kg, 30 μmol/kg, 100 μmol/kg; pre-injected 30 mins) elicits robust antihyperalgesia, while it shows no effect in IL-1alphabeta knockout mice.Furthermore, A 839977 attenuates dorsal horn neuronal responses in cancer-bearing animals.
• In Vitro:
  A 839977 selectively blocks BzATP-evoked calcium influx at mammalian P2X7 receptors (IC50=20-150 nM) and inhibits agonist-evoked YO-PRO uptake and IL-1beta release from differentiated human THP-1 cells. It has demonstrated efficacy in reducing inflammatory and neuropathic pain in animal models. Pre-treatment with A 839977 (50 nM for 1 hour) significantly prevents the pressure-induced rise of IL-1β priming in optic nerve astrocytes.

Storage & Handling

• Storage: store at low temperature | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

Ca(2+) receptor, Calcium Channel, A839977, A-839977, A 839977, CalciumChannel, mouse P2X7 receptor, human P2X7 receptor, P2X Receptor, P2X7, P2XReceptor, rat P2X7 receptor

Compound Identifiers

PubChem CID

53325875