Name: BCTC
Brand: Alomone Labs
SKU: B-110

Overview

Cat #: B-110

Alternative Name N-(4-tert-butylphenyl)-4-(3-chloropyridin-2-yl)piperazine-1-carboxamide

Lyophilized Powder yes

Source Synthetic

MW: 372.9

Purity: >99% (HPLC)

Effective concentration 1 nM – 100 nM.

Structure

Chemical name N-(4-tert-butylphenyl)-4-(3-chloropyridin-2-yl)piperazine-1-carboxamide.

Molecular formula C₂₀H₂₅ClN₄O.

CAS No.: 393514-24-4

PubChem CID 9929425

Activity BCTC is a potent and selective antagonist of TRPV1 channels, shown to inhibit capsaicin-, pH- and PKC-induced responses of mouse TRPV1 with IC₅₀ of 1.3, 0.59 and 0.37 nM, respectively.^1,2BCTC is also a blocker of TRPM8 channels, inhibiting rat TRPM8-mediated menthol and cold-evoked Ca²⁺ response with IC₅₀ of 0.6 µM.³

References-Activity

Vriens, J. et al. (2009) Mol. Pharmacol. 75, 1262.
Correll, C.C. et al. (2004) Neurosci. Lett. 370, 55.
Madrid, R. et al. (2006) J. Neurosci. 26, 12512.

Shipping and storage Shipped at room temperature. Product as supplied can be stored intact at room temperature for several weeks. For longer periods, it should be stored at -20°C.

Solubility 1-10 mM in DMSO. Centrifuge all product preparations before use (10000 x g 5 min).

Storage of solutions Up to four weeks at 4°C or three months at -20°C.

Our bioassay

Alomone Labs BCTC blocks TRPV1 channels expressed in C6 cells.
Pre-incubation with 0.1 nM, 1 nM and 10 nM BCTC (#B-110), as indicated, inhibits the 1 µM capsaicin (#C-125)-evoked rise in intracellular Ca²⁺ (control). mTRPV1-C6 cells were loaded with Fluo-3-AM. Changes in intracellular Ca²⁺ were detected as changes in Fluo-3 fluorescent emission following agonist application.

References - Scientific background

Vriens, J. et al. (2009) Mol. Pharmacol. 75, 1262.
McLeod, R.L. et al. (2006) Cough 2,10.
Horton, J.S. et al. (2013) Channels (Austin) 7, 17.

Scientific background

BCTC (N-(4-tertiarybutylphenyl)-4-(3-chloropyridin-2-yl)tetrahydropyrazine-1(2H)-carbox-amide) is a potent, selective antagonist of the vanilloid receptor 1 (TRPV1) that is orally bioavailable. BCTC has the ability to block the activation of TRPV1 by capsaicin and by low pH. It has an IC₅₀ of 35 nM³. Oral administration of BCTC in rats significantly reduces mechanical and thermal hyperalgesia associated with inflammation or nerve injury¹_.

TRPV1 is a member of a distinct subgroup of the transient receptor potential (TRP) ion channel family, highly expressed in primary nociceptors. TRPV1 can be activated by several different stimuli such as heat, acid, certain arachidonic acid derivatives and direct phosphorylation via PKC. TRPV1 may serve a central role in inflammatory nociception².

Several recent studies have showed that administration of BCTC in patients suffering from symptoms of cardiac hypertrophy and heart failure can overcome loss-of-heart function.

It has been suggested that TRPV1 blockade can be used as a new treatment strategy for cardiac hypertrophy and heart failure³.

Target TRPV1 and TRPM8 channels

Lyophilized Powder

BCTC (#B-110) is a highly pure, synthetic, and biologically active compound.

Certificate of Analysis SDS

For research purposes only, not for human use

Last Update: 07/05/2024

Applications

Citations

Electrophysiology

HEK 293 transfected cells.
McArthur, J.R. et al. (2019) Br. J. Pharmacol. 176, 2264.

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BCTC

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Scientific Background

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