Capsazepine 是一种 TRPV1 受体的拮抗剂， IC50值为 562 nM。 它可阻断由激活 TRPV1 离子通道的辣椒素引起的热痛感，是辣椒素拮抗剂。

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.

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)[1].

138977-28-3

C19H21ClN2O2S

376.9

DMSO:50 mg/mL (132.66 mM)
Powder: -20°C for 3 years
In solvent: -80°C for 2 years