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Cat. No. M6494
BCTC Structure
Size Price Availability Quantity
5mg USD 60  USD60 In stock
10mg USD 80  USD80 In stock
25mg USD 160  USD160 In stock
50mg USD 270  USD270 In stock
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Biological Activity

BCTC is a orally effective vanilloid receptor 1 (TRPV1 receptor) antagonist. BCTC is also a potent and specific inhibitor of transient receptor potential cation channel subfamily M member 8 (TRPM8) in prostate cancer (PCa) DU145 cells. BCTC inhibits acid- and capsaicin-induced activation of rat TRPV1 receptors (IC50 values are 6.0 and 35 nM respectively). BCTC displays analgesic properties in rat models of inflammatory and neuropathic pain.

Product Citations
Protocol (for reference only)
Cell Experiment
Cell lines
Preparation method
Incubation time
Animal Experiment
Animal models Jugular-cannulated male Sprague-Dawley rats (200-300 g)
Formulation using 25% hydroxypropyl-β-cyclodextrin as vehicle
Dosages 3, 10, and 40 mg/kg p.o. or 3 mg/kg i.v.
Administration p.o. or i.v.
Chemical Information
Molecular Weight 372.89
Formula C20H25ClN4O
CAS Number 393514-24-4
Solubility (25°C) DMSO ≥ 38 mg/mL
Storage Powder          -20°C   3 years ;  4°C   2 years
In solvent       -80°C   6 months ;  -20°C   1 month
Conversion of different model animals based on BSA (PMID: 27057123)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.


[1] Tao Liu, et al. Oncol Lett. Anti-tumor activity of the TRPM8 inhibitor BCTC in prostate cancer DU145 cells

[2] Kenneth J Valenzano, et al. J Pharmacol Exp Ther. 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

[3] Houlihan, et al. J Neurochem. Activity of cytisine and its brominated isoteres on recombinant human α7, α4β2 and α4β4 nicotinic acetylcholine receptors.

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Abmole Inhibitor Catalog

Keywords: BCTC supplier, TRP Channel, inhibitors, activators

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