Capsazepine Inhibitor

Capsazepine is an antagonist of TRPV1 receptor (IC50 : 562nM). 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.

1. Yang MH, Jung SH, Sethi G,et al.Pleiotropic Pharmacological Actions of Capsazepine, a Synthetic Analogue of Capsaicin, against Various Cancers and Inflammatory Diseases[J].Molecules. 2019 Mar 12;24 (5). pii: E995.
2. Sung B, Prasad S, Ravindran J, et al. Capsazepine, a TRPV1 antagonist, sensitizes colorectal cancer cells to apoptosis by TRAIL through ROS-JNK-CHOP-mediated upregulation of death receptors[J]. Free radical biology & medicine, 2012, 53 (10).
3. Cabral LD, et al. The Transient Receptor Potential Vanilloid 1 Antagonist Capsazepine Improves the Impaired Lung Mechanics during Endotoxemia. Basic Clin Pharmacol Toxicol. 2016 Nov;119 (5):421-427.

Small volumes of Capsazepine, inhibitor vial(s) may occasionally become entrapped in the seal of the product vial during shipment and storage. If necessary, briefly centrifuge the vial on a tabletop centrifuge to dislodge any liquid in the container`s cap. Certain products may require to ship with dry ice and additional dry ice fee may apply.

MBS5752383 is an inhibitor targeting Capsazepine.