AP-18

SKU: orb1306305

Description

AP-18 is a potent, selective TRPA1 antagonist, inhibiting cinnamaldehyde- and AITC-induced activation in vitro (IC50 ~3-10 µM). It demonstrates in vivo efficacy by reversing CFA-induced mechanical hyperalgesia in mice, making it a valuable research tool for studying pain and inflammation pathways.

Research Area

Neuroscience

Key Properties

• CAS Number: 55224-94-7
• MW: 209.7
• Purity: >98%
• Formula: C₁₁H₁₂ClNO
• SMILES: C\C(=C/c1ccc(Cl)cc1)\C(\C)=N\O
• Target: Ion channel
• Solubility: Soluble in DMSO (up to 25 mg/ml) or in Ethanol (up to 20 mg/ml).

Bioactivity

• Target IC50:
  TRPA1:~3 μM
• In Vivo:
  AP18 (1 mM; injected in the hindpaw of mice) effectively inhibits nociceptive events triggered by cinnamaldehyde, but not those induced by capsaicin, demonstrating its specificity and efficacy .
• In Vitro:
  At concentrations up to 50 μM, AP-18 does not significantly inhibit the activation of TRPV1, TRPV2, TRPV3, TRPV4, or TRPM8. However, it effectively and reversibly inhibits the activation of mouse TRPA1 by iodoacetamide (an irreversible cysteine-alkylating agent) in CHO cells, as determined through ratiometric Ca2+ imaging. Additionally, AP-18 prevents cold- and mustard-oil-triggered activation of mouse TRPA1 and inhibits TRPA1 currents induced by cinnamaldehyde in Xenopus oocyte excised patches, demonstrating its specificity and effectiveness in modulating TRPA1 activity .

Storage & Handling

• Storage: RT
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

dorsal, AP 18, AP18, AP-18, ganglia, hyperalgesia, Inhibitor, inhibit, pain, nociceptive, nerves, TRP Channel, TRPA1, TRPChannel, TRPV Channel, TRPVChannel, transduction, Transient receptor potential channels, root

Compound Identifiers

PubChem CID

9584673