BCTC

• CAT Number: I003440
• CAS Number: 393514-24-4
• Molecular Formula: C20H25ClN4O
• Molecular Weight: 372.9
• Purity: ≥95%
• Target: TRP Channel
• Solubility: 10 mM in DMSO
• Storage: Store at RT
• InChIKey: ROGUAPYLUCHQGK-UHFFFAOYSA-N

BCTC is a potent and specific inhibitor of transient receptor potential cation channel subfamily M member 8 (TRPM8) in prostate cancer (PCa) DU145 cells.Target: TRPM8in vitro: BCTC is a potent and specific antagonist of TRPM8, exerts an anti-tumor effect on the androgen-independent PCa DU145 cells, and the mechanism of how the inhibition functions. BCTC exerts an anti-proliferative effect on DU145 cells and induces tumor suppression through G0/G1 cell cycle arrest, and inhibition of migration and invasion. BCTC demonstrates excellent anti-tumor activity in PCa DU145 cells, and therefore has the potential to become a targeted therapeutic strategy against PCa. [1]in vivo: BCTC is a potent, selective, and orally bioavailable antagonist of rat VR1. BCTC not only blocks the activation of rat VR1 by capsaicin but also by low pH at the native rat VR1 in a skin-nerve preparation. Thus, BCTC has provided us with an opportunity to test our hypothesis that the inhibition of low pH induced activation of VR1 confers in vivo efficacy in models of chronic pain. This report describes the effects of BCTC in models of inflammatory, neuropathic, and capsaicin-induced pain in the rat. The efficacy and side effect profile of BCTC in these models were compared with those of nonsteroidal anti-inflammatory drugs and antiepileptic drugs currently used for the clinical therapy of inflammatory and neuropathic pain, respectively.[2]

Reference

1:Anti-tumor activity of the TRPM8 inhibitor BCTC in prostate cancer DU145 cells. Liu T, Fang Z, Wang G, Shi M, Wang X, Jiang K, Yang Z, Cao R, Tao H, Wang X, Zhou J.Oncol Lett. 2016 Jan;11(1):182-188. Epub 2015 Nov 2. PMID: 26870186 Free PMC Article2:Synthesis of Analogues of BCTC Incorporating a Pyrrolidinyl Linker and Biological Evaluation as Transient Receptor Potential Vanilloid 1 Antagonists. Yan L, Wang J, Pan M, Qiu Q, Huang W, Qian H.Chem Biol Drug Des. 2016 Feb;87(2):306-11. doi: 10.1111/cbdd.12661. Epub 2015 Oct 5. PMID: 26360809 3:Use and limitations of three TRPV-1 receptor antagonists on smooth muscles of animals and man: a vote for BCTC. Benko R, Illényi L, Kelemen D, Papp R, Papp A, Bartho L.Eur J Pharmacol. 2012 Jan 5;674(1):44-50. doi: 10.1016/j.ejphar.2011.10.021. Epub 2011 Oct 25. PMID: 22056835 4:Effect of transient receptor potential vanilloid 1 (TRPV1) receptor antagonist compounds SB705498, BCTC and AMG9810 in rat models of thermal hyperalgesia measured with an increasing-temperature water bath. Tékus V, Bölcskei K, Kis-Varga A, Dézsi L, Szentirmay E, Visegrády A, Horváth C, Szolcsányi J, Petho G.Eur J Pharmacol. 2010 Sep 1;641(2-3):135-41. doi: 10.1016/j.ejphar.2010.05.052. Epub 2010 Jun 8. PMID: 20534382 5:N-(4-tertiarybutylphenyl)-4-(3-chloropyridin-2-yl)tetrahydropyrazine -1(2H)-carbox-amide (BCTC), a novel, orally effective vanilloid receptor 1 antagonist with analgesic properties: I. in vitro characterization and pharmacokinetic properties. Valenzano KJ, Grant ER, Wu G, Hachicha M, Schmid L, Tafesse L, Sun Q, Rotshteyn Y, Francis J, Limberis J, Malik S, Whittemore ER, Hodges D.J Pharmacol Exp Ther. 2003 Jul;306(1):377-86. Epub 2003 Apr 29. PMID: 12721338 Free Article6:N-(4-Tertiarybutylphenyl)-4-(3-cholorphyridin-2-yl)tetrahydropyrazine -1(2H)-carbox-amide (BCTC), a novel, orally effective vanilloid receptor 1 antagonist with analgesic properties: II. in vivo characterization in rat models of inflammatory and neuropathic pain. Pomonis JD, Harrison JE, Mark L, Bristol DR, Valenzano KJ, Walker K.J Pharmacol Exp Ther. 2003 Jul;306(1):387-93. Epub 2003 Apr 29. PMID: 12721336 Free Article