BCTC

Product details

• Chemical name: N-(4-tert-butylphenyl)-4-(3-chloropyridin-2-yl)piperazine-1-carboxamide.
• Also known as: N-(4-tert-butylphenyl)-4-(3-chloropyridin-2-yl)piperazine-1-carboxamide
• CAS number: 393514-24-4
• Molecular formula: C20H25ClN4O.
• Purity: >99% (HPLC)
• Concentration: 1 nM - 100 nM.
• Form: Lyophilized Powder
• Solubility: 1-10 mM in DMSO. Centrifuge all product preparations before use (10000 x g 5 min).
• Reconstitution: Centrifuge the vial before adding solvent (10,000 x g for 5 minutes) to spin down all the powder to the bottom of the vial. The lyophilized product may be difficult to visualize. Add solvent directly to the centrifuged vial. Tap the vial to aid in dissolving the lyophilized product. Tilt and gently roll the liquid over the walls of the vial. Avoid vigorous vortexing. Light vortexing for up to 3 seconds is acceptable if needed. For long-term storage in solution, we recommend preparing a stock solution by dissolving the product in sterile water at a concentration of at least 0.1 mg/mL. Divide the stock solution into small aliquots and store at -20°C. Before use, thaw the relevant vial(s) and dilute to the desired working concentration in your working buffer. It is recommended to prepare fresh solutions in working buffers just before use. Repeat freeze-thawing may result in loss of activity
• Shipping: 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.
• Target: TRPV1 and TRPM8 channels
• Source: Synthetic
• 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.1,2 BCTC is also a blocker of TRPM8 channels, inhibiting rat TRPM8-mediated menthol and cold-evoked Ca2+ response with IC50 of 0.6 µM.3
• Alternative names: N-(4-tert-butylphenyl)-4-(3-chloropyridin-2-yl)piperazine-1-carboxamide

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.

Lead time: 1-2 Business Days

Country of origin: Israel/IL

Applications key

Application key: FC- Flow cytometry, IFC- Indirect flow cytometry, IHC- Immunohistochemistry,LCI- Live cell imaging, Calcium imaging assay,Cell survival assay, Electrophysiology, Neurite outgrowth assay.

Bioassay tested: Yes

• SDS (PDF)

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