HC-030031

SKU: orb1300688

Description

HC-030031

Research Area

Pharmacology & Drug Discovery

Key Properties

• CAS Number: 349085-38-7
• MW: 355.39
• Purity: 99.69%
• Formula: C₁₈H₂₁N₅O₃
• SMILES: CC(C)c1ccc(NC(=O)Cn2cnc3n(C)c(=O)n(C)c(=O)c23)cc1
• Target: TRP/TRPV Channel
• Solubility: DMSO:35.5 mg/mL (99.89 mM)

Bioactivity

• Target IC50:
  Ca2+ influx (AITC-evoked):6. ± .2 μM|Ca2+ influx (formalin-evoked):5. ± .2 μM
• In Vivo:
  HC-030031 rapidly inhibits both inward and outward currents induced by AITC or Formalin, and also suppresses TRPA1 activation caused by N-methy Maleimide and electrophilic prostag andins.
• In Vitro:
  Oral administration of HC-030031 (100 mg/kg) significantly reversed Mechanical hypersensitivity in rat models of chronic inflammation or neuropathic pain, while local injection (100 μg) int the inflamed hind paw of mice attenuated Mechanical , but not thermal, hypersensitivity.
• Cell Research:
  HC-030031 is prepared in DMSO and stored, and then diluted with appropriate medium (DMSO 0.4%) before us. HEK-293 cells stably expressing human TRPA1 are plated into 384-well plates at a density of 20,000 cells/well 24 hours prior to assaying. O the day of assay, cells are loaded with 4 μM Fluo-4 dye and 0.08% pluronic acid for 1 hour at room temperature in assay buffer consisting of Hank's balanced salt solution supplemented with 20 mM HEPES, 2.5 mM probenecid, and 4% TR-40. Calcium influx assays are performed usin the Fluorometric Imaging Plate Reader (FLIPR) TETRA. concentration response curves are generated fo the TRPA1 agonists cinnamaldehyde and AITC prior to antagonist testing so EC60 concentration could be determined. Titrations of HC-030031 are made from a DMSO stock solution and DMSO is kept to a constant of 0.4% in the assay the antagonist is incubated wit the cells for 10 minutes befor the addition of an EC60 concentration of either cinnamaldehyde (18 μM) or AITC (6 μM) and calcium influx is monitored for an additional 10 minute.
• Animal Research:
  Animal Models: Male Sprague Dawley rats. Formulation: 0.5% Methylcellulose. Dosages: 100,300 mg/kg. Administration: oral administration

Storage & Handling

• Storage: Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
• Disclaimer: For research use only

Alternative Names

TOSLAB 829227, TOSLAB829227, TOSLAB-829227, Transient receptor potential channels, TRPA1, TRP Channel, TRPChannel, TRPV Channel, TRPVChannel, Inhibitor, HC 030031, HC030031, HC-030031, inhibit

Compound Identifiers

PubChem CID

1150897