Capsazepine

SKU: orb1220535

Description

Capsazepine is an antagonist of TRPV1 receptor ( IC50 : 562 nM). Capsazepine blocks the painful sensation of heat caused by capsaicin (the active ingredient of chilli pepper) which activates the TRPV1 ion channel. It is therefore considered to be a capsaicin antagonist.

Key Properties

• CAS Number: 138977-28-3
• MW: 376.9
• Purity: >98% (HPLC)
• Formula: C₁₉H₂₁ClN₂O₂S
• SMILES: Oc1cc2CCCN(Cc2cc1O)C(=S)NCCc1ccc(Cl)cc1
• Target: TRP/TRPV Channel
• Solubility: DMSO:50 mg/mL (132.66 mM)

Bioactivity

• In Vivo:
  Capsazepine (15 mg/kg, s. c.) prevents the increase in respiratory system resistance and decreases the increase in tissue damping during endotoxemia. Capsazepine attenuates lung injury evidenced by reduction on collapsed area of the lung parenchyma induced by LPS.
• In Vitro:
  Capsazepine (50 μM) optimally enhances the upregulation of (death receptors) DRs without affecting cell viability HCT116 cells. Capsazepine (30-50 μM) induces ROS generation and ROS mediate Capsazepine-induced DR5 upregulation in HCT116 cells. Capsazepine (1-100 μM, 45 min preincubation) inhibits the evoked CGRP-LI release. Capsazepine (3-100 μM) prevents low pH- and capsaicin-induced CGRP-LI release from rat soleus muscle at concentrations which do not affect the release evoked by KCl. Capsazepine (3-100 μM, without 10 μM) produces a nonspecific inhibitory effect on CGRP-LI release from peripheral endings of the capsaicin-sensitive primary afferent neurone.

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

TRP/TRPV Channel