BCTC

BCTC is an orally active current inhibitor of vanilloid receptor type 1 (VR1). BCTC is a transient receptor potential cation channel subfamily M member 8 (TRPM8) and transient receptor potential vanilloid 1 (TRPV1) antagonist. BCTC is an insulin sensitizer and secretor. BCTC has anticancer and analgesic effects^{[1][2][3][4][5]}. IC50 & Target:IC50: 37.0 nM (CGRP-LI)^[3].
IC50: 36.0 nM (SP-LI)^[3].
In Vitro:BCTC (20-100 μM; 72 h) shows highly selective antitumor activity in DU145 cells^[1].
BCTC (20-100 μM; 48 h) induces cell cycle arrest in the G0/G1 phase by selectively regulating the expression levels of cell cycle regulatory protein subsets, and doesn’t induce apoptosis^[1].
BCTC (10 μM and 100 μM; 48 h) inhibits cell migration and invasion^[1].
BCTC effectively inhibits the TRPV1 function of rat spinal cord by inhibiting the release of calcitonin gene-related peptide-like immunoreactivity (CGRP-LI) (IC₅₀=37.0 nM) and P-like substance immunoreactivity (SP-LI) (IC₅₀=36.0 nM) induced by capsaicin (300 nM) ^[3].
In Vivo:BCTC (1-30 mg/kg; Oral gavage; Single dose) can inhibit inflammatory and neuropathic heat pain and mechanical hyperalgesia in Sprague-Dawley rats by targeting VR1, which has analgesic effect^[2].
BCTC (10-100 mg/kg; Oral gavage, Twice daily for 4 weeks) improves the insulin resistance and systemic glucose and lipid metabolism, and increase insulin secretion in diabetic ob/ob mice^[5].