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BCTC

Cat. No. M6494
BCTC Structure
Size Price Availability Quantity
5mg USD 72  USD80 In stock
10mg USD 108  USD120 In stock
50mg USD 360  USD400 In stock
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Quality Control
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.

Protocol
Cell Experiment
Cell lines
Preparation method
Concentrations
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.
Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)
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.

Chemical Information
Molecular Weight 372.89
Formula C20H25ClN4O
CAS Number 393514-24-4
Purity 99.96%
Solubility DMSO ≥ 38 mg/mL
Storage at -20°C
References

Anti-tumor activity of the TRPM8 inhibitor BCTC in prostate cancer DU145 cells
Tao Liu, et al. Oncol Lett. 2016 Jan;11(1):182-188. PMID: 26870186.

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
Kenneth J Valenzano, et al. J Pharmacol Exp Ther. 2003 Jul;306(1):377-86. PMID: 12721338.

Activity of cytisine and its brominated isoteres on recombinant human α7, α4β2 and α4β4 nicotinic acetylcholine receptors.
Houlihan, et al. J Neurochem. 2001;78: 1029. PMID: 11553677.

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  Catalog
Abmole Inhibitor Catalog 2017




Keywords: BCTC supplier, TRP Channel, inhibitors

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