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MedChemExpress - Model BCTC - 393514-24-4

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].

BCTC

MCE China：BCTC

Brand：MedChemExpress (MCE)

Cat. No.HY-19960

CAS：393514-24-4

Purity：98.03%

Storage：Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year

Shipping：Room temperature in continental US; may vary elsewhere.

Description：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.

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].

IC50 & Target：IC50: 37.0 nM (CGRP-LI)[3]. IC50: 36.0 nM (SP-LI)[3]. Cellular Effect Cell Line Type Value Description References

References：

[1]. Liu T, et al. Anti-tumor activity of the TRPM8 inhibitor BCTC in prostate cancer DU145 cells. Oncol Lett. 2016 Jan;11(1):182-188. [Content Brief]

[2]. Pomonis JD, et al. 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. J Pharmacol Exp Ther. 2003 Jul;306(1):387-93. [Content Brief]

[3]. Kanai Y, et al. Involvement of an increased spinal TRPV1 sensitization through its up-regulation in mechanical allodynia of CCI rats. Neuropharmacology. 2005 Dec;49(7):977-84. [Content Brief]

[4]. Nie C, et al. Study on chemical modification and analgesic activity of N-(4-tert-butylphenyl)-4-(3-chloropyridin-2-yl) piperazine-1-carboxamide. Eur J Med Chem. 2020 May 15;194:112236. [Content Brief]

[5]. Tanaka H, et al. Enhanced insulin secretion and sensitization in diabetic mice on chronic treatment with a transient receptor potential vanilloid 1 antagonist. Life Sci. 2011 Mar 14;88(11-12):559-63. [Content Brief]

Brand introduction:
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