Capsazepine

SKU: orb1300007

Description

Capsazepine is a selective TRPV1 receptor antagonist (IC50 = 562 nM) that inhibits capsaicin-induced activation. It is widely used in neuroscience and pain research to study thermal nociception and inflammatory pathways in both in vitro cellular assays and in vivo animal models.

Research Area

Cell Biology, Pharmacology & Drug Discovery

Key Properties

• CAS Number: 138977-28-3
• MW: 376.9
• Purity: 99.78% (May vary between batches)
• Formula: C₁₉H₂₁ClN₂O₂S
• SMILES: Oc1cc2CCCN(Cc2cc1O)C(=S)NCCc1ccc(Cl)cc1
• Target: Apoptosis,TRP/TRPV Channel
• Solubility: DMSO:104 mg/mL (275.94 mM);10% DMSO+40% PEG300+5% Tween 80+45% Saline:5 mg/mL (13.27 mM)

Bioactivity

• Target IC50:
  TRPA1:562 nM
• In Vivo:
  Capsazepine is a synthetic analogue of capsaicin that can function as an antagonist of TRPV1. Capsazepine can exhibit diverse effects on cancer (prostate cancer, breast cancer, colorectal cancer, oral cancer, and osteosarcoma) growth and survival, and can be therapeutically used against other major disorders such as colitis, pancreatitis, malaria, and epilepsy. Capsazepine has been reported to exhibit pleiotropic anti-cancer effects against numerous tumor cell lines. Capsazepine can modulate Janus activated kinase (JAK)/signal transducer and activator of the transcription (STAT) pathway, intracellular Ca2+ concentration, and reactive oxygen species (ROS)-JNK-CCAAT/enhancer-binding protein homologous protein (CHOP) pathways. It can inhibit cell proliferation, metastasis, and induce apoptosis. Moreover, capsazepine can exert anti-inflammatory effects through the downregulation of lipopolysaccharide (LPS)-induced nuclear transcription factor-kappa B (NF-κB), as well as the blockage of activation of both transient receptor potential cation channel subfamily V member 1 (TRPV1) and transient receptor potential cation channel, subfamily A, and member 1 (TRPA1).

Storage & Handling

• Storage: store at low temperature,keep away from direct sunlight | 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

Transient receptor potential channels, TRPV Channel, TRPVChannel, TRPChannel, TRPA1, TRP Channel, Capsazepine, Apoptosis, Inhibitor, inhibit

Compound Identifiers

PubChem CID

2733484