A-967079

SKU: orb1299980

Description

A 967079 is a potent, selective, and bioavailable small molecule TRPA1 channel blocker, demonstrating IC50 values of 67 nM (human) and 289 nM (rat). It is widely used in vitro and in vivo to investigate TRPA1's role in pain, inflammation, and respiratory disorders.

Research Area

Pharmacology & Drug Discovery

Key Properties

• CAS Number: 1170613-55-4
• MW: 207.24
• Purity: >99.99% (May vary between batches)
• Formula: C₁₂H₁₄FNO
• SMILES: CC\C(=N/O)\C(\C)=C\c1ccc(F)cc1
• Target: TRP/TRPV Channel
• Solubility: 10% DMSO+40% PEG300+5% Tween 80+45% Saline:4 mg/mL (19.3 mM);DMSO:100 mg/mL (482.53 mM)

Bioactivity

• Target IC50:
  TRPA1 receptor (human):67 nM (IC50)|TRPA1 receptor (rat):289 nM (IC50)
• In Vivo:
  Systemic injection of A 967079 (30 micromol/kg) decreased the responses of wide dynamic range (WDR), and nociceptive specific (NS) neurons following noxious pinch stimulation of the ipsilateral hind paw in uninjured and CFA-inflamed rats. Similarly, A-967079 reduced the responses of WDR neurons to high-intensity mechanical stimulation (300 g von Frey hair) of the knee joint in both OA and OA-sham rats. WDR neuronal responses to low-intensity mechanical stimulation (10 g von Frey hair) were also reduced by A-967079 administration to CFA-inflamed rats, but no effect was observed in uninjured rats. Additionally, the spontaneous activity of WDR neurons was decreased after A-967079 injection in CFA-inflamed rats but was unaltered in uninjured, OA, and OA-sham animals.
• Animal Research:
  Separated by 5 min each, to specific stimulation of the neuronal RF were recorded. Spontaneous and evoked neuronal activity was then measured 5, 15, 25, and 35 min after systemic injection of A-967079 (30 μmol/kg) or vehicle (polyethylene glycol). The intravenous injection of A-967079 or vehicle was completed over a 6-7 min period. The i.v. dose of A-967079 was selected based on extrapolated plasma levels that were effective in behavioral studies . Except for 2 experiments in which two easily distinguished neurons were simultaneously recorded on one electrode, only one neuron was studied per rat. Since only one vehicle was used in these experiments, vehicle data was combined when a clear "no effect' was observed in at least 2-3 animals from a particular subset of groups (OA and sham OA).

Storage & Handling

• Storage: 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

A967079, A-967079, A 967079, inhibit, Inhibitor, Transient receptor potential channels, TRPV Channel, TRPVChannel, TRP Channel, TRPA1, TRPChannel

Compound Identifiers

PubChem CID

42641861