A 839977

SKU: orb2901640

Description

A 839977 is a P2X7 selective antagonist; it blocks BzATP-evoked calcium influx at recombinant human, rat and mouse P2X7 receptors (IC50 values are 20 nM, 42 nM and 150 nM respectively) and reduces inflammatory and neuropathic pain in animal models; the antihyperalgesic effects of P2X7 receptor blockadeare mediated by blocking the release of IL-1beta.

Key Properties

• CAS Number: 870061-27-1
• MW: 413.26
• Purity: >98% (HPLC)
• Formula: C₁₉H₁₄Cl₂N₆O
• SMILES: Clc1cccc(c1Cl)-n1nnnc1NCc1ccccc1Oc1ccccn1
• Target: Calcium Channel
• Solubility: In Vitro: DMSO : 100 mg/mL (241.98 mM; Ultrasonic )

Bioactivity

• In Vivo:
  A 839977 (30 μmol/kg, 100 μmol/kg, 300 μmol/kg; pre-injected 30mins) dose-dependently reduces thermal hyperalgesia produced by intraplantar administration of complete Freund's adjuvant (CFA) in rats. A 839977 (10 μmol/kg, 30 μmol/kg, 100 μmol/kg; pre-injected 30mins) produces robust antihyperalgesia in the CFA model of inflammatory pain in wild-type mice, but it has no effect on IL-1alphabeta knockout mice. A 839977 attenuates dorsal horn neuronal responses in cancer bearing animals. Animal model: Male Sprague-Dawley, BALB/c mice and IL-1 (/) mice for CFA-induced chronic inflammatory. Dosage: 30 μmol/kg, 100 μmol/kg, 300 μmol/kg (rat); 10 μmol/kg, 30 μmol/kg, 100 μmol/kg (mice). Administration: Injection; pre-injected 30mins. Result: Attenuated CFA-induced thermal hyperalgesia in a dose-related manner in rat and mice, but has no effect on IL-1 (/) mice.
• In Vitro:
  A 839977 selectively blocks BzATP-evoked calcium influx at mammalian P2X7 receptors, (IC50 = 20-150 nM), which blocks agonist-evoked YO-PRO uptake and IL-1beta release from differentiated human THP-1 cells, it has been shown to reduce inflammatory and neuropathic pain in animal models. A 839977 (50 nM, pre-treatment 1 hour) significantly prevents pressure-induced rise of IL-1β priming in optic nerve astrocytes. RT-PCR Cell line: Optic nerve astrocyte cells. Concentration: 50 nM. Incubation time: 1 hour(pre-treatment). Result: Prevented the IL-1β priming in astrocyte cells

Storage & Handling

• Storage: Storage temperature: -20°C. Stability: ≥ 2 years
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Quick Database Links

Gene Symbol

Calcium Channel