Cat. No.: HY-19960

BCTC

5 Cited Publications

Customer Review

Based on 5 publication(s) in Google Scholar

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.

For research use only. We do not sell to patients.

Purity: 99.66%
CAS No.: 393514-24-4
Formula: C₂₀H₂₅ClN₄O
Molecular Weight:372.89

Storage:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year

BCTC Chemical Structure

CAS No.: 393514-24-4

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Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biological Activity
- Description
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
- Clinical Trial
Chemical Information
Publications (5)
Solvent & Solubility
- In Vitro
- In Vivo
Purity & Documentation
References
Help & FAQs
Classifications
Bioz

Biological Activity

Description

IC₅₀ & Target

IC50: 37.0 nM (CGRP-LI)^[3].
IC50: 36.0 nM (SP-LI)^[3].

All TRP Channel Isoforms :

Cellular Effect

Cell Line	Type	Value	Description	References
CHO	IC₅₀	0.4 nM Compound: 4	Antagonist activity against capsaicin-induced 45calcium ion uptake in CHO cells expressing rat TRPV1 Antagonist activity against capsaicin-induced 45calcium ion uptake in CHO cells expressing rat TRPV1	[PMID: 16759115]
CHO	IC₅₀	0.5 nM Compound: 5	Antagonist activity at rat TRPV1 expressed in CHO cells assessed as blockade of capsaicin-induced receptor activation by [45Ca2+] uptake assay Antagonist activity at rat TRPV1 expressed in CHO cells assessed as blockade of capsaicin-induced receptor activation by [45Ca2+] uptake assay	[PMID: 17489570]
CHO	IC₅₀	0.5 nM Compound: 4	Antagonist activity against acid-induced 45calcium ion uptake in CHO cells expressing rat TRPV1 at pH5 Antagonist activity against acid-induced 45calcium ion uptake in CHO cells expressing rat TRPV1 at pH5	[PMID: 16759115]
CHO	IC₅₀	0.6 nM Compound: 5	Antagonist activity at human TRPV1 expressed in CHO cells assessed as blockade of capsaicin-induced receptor activation by [45Ca2+] uptake assay Antagonist activity at human TRPV1 expressed in CHO cells assessed as blockade of capsaicin-induced receptor activation by [45Ca2+] uptake assay	[PMID: 17489570]
CHO	IC₅₀	0.7 nM Compound: 5	Antagonist activity at human TRPV1 expressed in CHO cells assessed as blockade of acid-induced receptor activation by [45Ca2+] uptake assay Antagonist activity at human TRPV1 expressed in CHO cells assessed as blockade of acid-induced receptor activation by [45Ca2+] uptake assay	[PMID: 17489570]
CHO	IC₅₀	0.7 nM Compound: 5	Antagonist activity at rat TRPV1 expressed in CHO cells assessed as blockade of acid-induced receptor activation by [45Ca2+] uptake assay Antagonist activity at rat TRPV1 expressed in CHO cells assessed as blockade of acid-induced receptor activation by [45Ca2+] uptake assay	[PMID: 17489570]
CHO-K1	IC₅₀	0.019 μM Compound: BCTC	Antagonist activity at capsaicin-induced human recombinant TRPV1 expressed in CHO-K1 cells co-expressing aequorin incubated for 2.5 mins in presence of ATP followed by capsaicin addition by luminescence assay Antagonist activity at capsaicin-induced human recombinant TRPV1 expressed in CHO-K1 cells co-expressing aequorin incubated for 2.5 mins in presence of ATP followed by capsaicin addition by luminescence assay	[PMID: 31202991]
HEK293	EC₅₀	4.5 μM Compound: BCTC	Antagonist activity at human TRPA1 expressed in HEK293 cells assessed as decrease in intracellular calcium level Antagonist activity at human TRPA1 expressed in HEK293 cells assessed as decrease in intracellular calcium level	[PMID: 19875281]
HEK293	IC₅₀	0.0067 μM Compound: BCTC	Antagonist activity at human TRPV1 expressed in HEK293 cells assessed as decrease in intracellular calcium level Antagonist activity at human TRPV1 expressed in HEK293 cells assessed as decrease in intracellular calcium level	[PMID: 19875281]
HEK293	IC₅₀	0.6 nM Compound: 5	Antagonist activity at human TRPV1 expressed in HEK293 cells assessed as blockade of acid-induced receptor activation by FLIPR assay Antagonist activity at human TRPV1 expressed in HEK293 cells assessed as blockade of acid-induced receptor activation by FLIPR assay	[PMID: 17489570]
HEK293	IC₅₀	0.6 nM Compound: 5	Antagonist activity at rat TRPV1 expressed in HEK293 cells assessed as blockade of acid-induced receptor activation by FLIPR assay Antagonist activity at rat TRPV1 expressed in HEK293 cells assessed as blockade of acid-induced receptor activation by FLIPR assay	[PMID: 17489570]
HEK293	IC₅₀	1.9 nM Compound: 5	Antagonist activity at rat TRPV1 expressed in HEK293 cells assessed as blockade of capsaicin-induced receptor activation by FLIPR assay Antagonist activity at rat TRPV1 expressed in HEK293 cells assessed as blockade of capsaicin-induced receptor activation by FLIPR assay	[PMID: 17489570]
HEK293	IC₅₀	29.8 nM Compound: BCTC	Inhibition of human vanilloid receptor 1 in HEK293 cells in pH 5.5-induced FLIPR assay Inhibition of human vanilloid receptor 1 in HEK293 cells in pH 5.5-induced FLIPR assay	[PMID: 15482915]
HEK293	IC₅₀	34 nM Compound: BCTC	Inhibition of human vanilloid receptor 1 in HEK293 cells in capsaicin-induced FLIPR assay Inhibition of human vanilloid receptor 1 in HEK293 cells in capsaicin-induced FLIPR assay	[PMID: 15482915]
HEK293	IC₅₀	34.9 nM Compound: 18	Vanilloid receptor subtype 1 antagonist activity based on its ability to block capsaicin-induced (CAP) activation of the rat VR1 channel in a HEK293 cell line Vanilloid receptor subtype 1 antagonist activity based on its ability to block capsaicin-induced (CAP) activation of the rat VR1 channel in a HEK293 cell line	[PMID: 14505681]
HEK293	IC₅₀	4.8 nM Compound: 18	Vanilloid receptor subtype 1 antagonist activity based on its ability to block low pH-induced activation of the rat VR1 channel in a HEK293 cell line Vanilloid receptor subtype 1 antagonist activity based on its ability to block low pH-induced activation of the rat VR1 channel in a HEK293 cell line	[PMID: 14505681]
HEK293	IC₅₀	475 nM Compound: BCTC	Antagonist activity at rat TRPM8 expressed in HEK293 cells assessed as inhibition of menthol mediated current amplitude at +80 mV holding potential by whole cell patch-clamp assay Antagonist activity at rat TRPM8 expressed in HEK293 cells assessed as inhibition of menthol mediated current amplitude at +80 mV holding potential by whole cell patch-clamp assay	[PMID: 26847872]
HEK293	IC₅₀	5 nM Compound: 5	Antagonist activity at human TRPV1 expressed in HEK293 cells assessed as blockade of capsaicin-induced receptor activation by FLIPR assay Antagonist activity at human TRPV1 expressed in HEK293 cells assessed as blockade of capsaicin-induced receptor activation by FLIPR assay	[PMID: 17489570]
HEK-293T	IC₅₀	0.15 nM Compound: BCTC	Antagonist activity at human brain TRPV1 expressed in HEK293T cells assessed as inhibition of CAP-induced intracellular Ca2+ influx by fluorescence-based assay Antagonist activity at human brain TRPV1 expressed in HEK293T cells assessed as inhibition of CAP-induced intracellular Ca2+ influx by fluorescence-based assay	[PMID: 24484240]
HEK-293T	IC₅₀	2.12 nM Compound: BCTC	Antagonist activity at rat TRPV1 receptor expressed in HEK293T cells assessed as inhibition of temperature-induced calcium flux after 30 mins by Fluo-4AM based fluorescence assay Antagonist activity at rat TRPV1 receptor expressed in HEK293T cells assessed as inhibition of temperature-induced calcium flux after 30 mins by Fluo-4AM based fluorescence assay	[PMID: 23796768]
HEK-293T	IC₅₀	4.86 nM Compound: BCTC	Antagonist activity at rat TRPV1 receptor expressed in HEK293T cells assessed as inhibition of capsaicin-induced calcium flux after 30 mins by Fluo-4AM based fluorescence assay Antagonist activity at rat TRPV1 receptor expressed in HEK293T cells assessed as inhibition of capsaicin-induced calcium flux after 30 mins by Fluo-4AM based fluorescence assay	[PMID: 23796768]

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].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Western Blot Analysis^[1]

Cell Line:

DU145
Concentration:

20 μM, 40 μM, 60 μM, 80 μM,100 μM
Incubation Time:

48 h
Result:

Down-regulated p-Akt, while p-GSK-3β was up-regulated leaving their unphosphorylated form unchanged.
Significantly down-regulated Cyclin D1(20), the most relevant protein in the cell cycle, without affecting cyclin-B1.
Reduced the expression of CDK2 and CDK6, but without affecting the expression level of CDK4.
Downregulates MMP2 and p-FAK levels.

Cell Viability Assay^[1]

Cell Line:

DU145, PNT1A
Concentration:

20 μM, 40 μM, 60 μM, 80 μM,100 μM
Incubation Time:

72 h
Result:

Decreased the growth of DU145 cells in a concentration-dependent manner, with 12.03% and 50.69% growth inhibition at 10 µM and 100 µM, respectively, but had little effect on normal prostate PNT1A cells.

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].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:

Capsaicin-induced Sprague-Dawley rats model^[2]
Dosage:

1 mg/kg, 3 mg/kg, 10 mg/kg, 30 mg/kg
Administration:

Oral gavage (p.o.), Single dose. Before capsaicin (HY-10448) treatment (30 μg; intraplantar injection; Single dose)
Result:

Inhibited capsaicin-mediated thermal hyperalgesia in a dose-dependent manner.

Animal Model:

Freund’s complete adjuvant (FCA) Sprague-Dawley rats model^[2]
Dosage:

1 mg/kg, 3 mg/kg, 10 mg/kg, 30 mg/kg
Administration:

Oral gavage (p.o.), Single dose. After 100 % FAC treatment (50 μL; intraplantar injection; Single dose)
Result:

Significantly reduced FAC-induced inflammation-related thermal pain and mechanical hyperalgesia, and extended the inhibitory effect of mechanical hyperalgesia to 6 h at high doses (10 mg/kg, 30 mg/kg).

Animal Model:

Partial sciatic nerve ligation Sprague-Dawley rats model^[2]
Dosage:

1 mg/kg, 3 mg/kg, 10 mg/kg, 30 mg/kg
Administration:

Oral gavage (p.o.), Single dose. After partial sciatic nerve ligation.
Result:

Reduced post-operative abnormal tactile pain and mechanical hyperalgesia in a dose-dependent manner.

Animal Model:

Particularly strong insulin resistance and hyperinsulinemia ob/ob mice model^[5]
Dosage:

10 mg/kg, 30 mg/kg, 100 mg/kg
Administration:

Oral gavage (p.o.); Twice daily for 4 weeks
Result:

Reduced plasma triglyceride and glucose area under the curve (AUC) level.
Decreased calcitonin gene-related peptide (CGRP) levels in a dose-dependent manner.

Clinical Trial

NCT Number	Sponsor	Condition	Start Date	Phase A549
NCT01329991	Plexxikon\|		2011-05	PHASE1

Chemical Information

CAS No. 393514-24-4
Appearance Solid
Molecular Weight 372.89
Formula C₂₀H₂₅ClN₄O
Color White to off-white
SMILES

O=C(N1CCN(C2=NC=CC=C2Cl)CC1)NC3=CC=C(C(C)(C)C)C=C3
Shipping

Room temperature in continental US; may vary elsewhere.

Storage

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

Publications (5)

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Nat Biomed Eng

Solvent-mediated analgesia via the suppression of water permeation through TRPV1 ion channels. [Abstract]

2025 Jun;9(6):905-916. PMID: 39572786
Phytomedicine

Capsaicin ameliorates cholestasis through modulation of the FXR-SHP and FXR-FGF15 gut-liver axis in mice. [Abstract]

2025 Oct:146:157130. PMID: 40782765
Brain Stimul

Focused magnetic stimulation for motor recovery after stroke. [Abstract]

2024 Sep-Oct;17(5):1048-1059. PMID: 39214184
J Toxicol Sci

Transient Receptor Potential Melastatin 8, a sensor of cold temperatures mediates expression of cyclin-dependent kinase inhibitor, p21/Cip1, a regulator of epidermal cell proliferation. [Abstract]

2022;47(3):117-123. PMID: 35236803
Fundam Toxicol Sci

2023;410(1):1-6.

Solvent & Solubility

In Vitro:

DMSO : ≥ 50 mg/mL (134.09 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

* "≥" means soluble, but saturation unknown.

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

2.6818 mL

13.4088 mL

26.8176 mL

5 mM

0.5364 mL

2.6818 mL

5.3635 mL

10 mM

0.2682 mL

1.3409 mL

2.6818 mL

Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.

Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Molarity Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

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Molecular Weight Molecular Weight

Dilution Calculator

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

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In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

Stock Solution Working Solution

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)

Solubility: ≥ 2.5 mg/mL (6.70 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

Protocol 2

Add each solvent one by one: 10% DMSO 90% Corn Oil

Solubility: ≥ 2.5 mg/mL (6.70 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
Saline +

The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Working solution concentration: 0.22 mg/mL

Purity & Documentation

Select Batch:

Purity: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (282 KB)
SDS (396 KB)
- English - EN (396 KB)
- Français - FR (396 KB)
- Deutsch - DE (396 KB)
- Norwegian - NO (396 KB)
- Español - ES (396 KB)
- Swedish - SV (396 KB)
- Italian - IT (396 KB)
- Korean - KR (396 KB)
- Portuguese - PT (396 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

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]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	2.6818 mL	13.4088 mL	26.8176 mL	67.0439 mL
	5 mM	0.5364 mL	2.6818 mL	5.3635 mL	13.4088 mL
	10 mM	0.2682 mL	1.3409 mL	2.6818 mL	6.7044 mL
	15 mM	0.1788 mL	0.8939 mL	1.7878 mL	4.4696 mL
	20 mM	0.1341 mL	0.6704 mL	1.3409 mL	3.3522 mL
	25 mM	0.1073 mL	0.5364 mL	1.0727 mL	2.6818 mL
	30 mM	0.0894 mL	0.4470 mL	0.8939 mL	2.2348 mL
	40 mM	0.0670 mL	0.3352 mL	0.6704 mL	1.6761 mL
	50 mM	0.0536 mL	0.2682 mL	0.5364 mL	1.3409 mL
	60 mM	0.0447 mL	0.2235 mL	0.4470 mL	1.1174 mL
	80 mM	0.0335 mL	0.1676 mL	0.3352 mL	0.8380 mL
	100 mM	0.0268 mL	0.1341 mL	0.2682 mL	0.6704 mL

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BCTC

Anti-diabetic Compound Library

Orally Active Compound Library

Mechanoreceptors Compound Library

Human Metabolite Library

Pain-Related Compound Library

Metabolic Enzyme Compound Library

Membrane Protein-targeted Compound Library

Membrane Receptor-targeted Compound Library

Mitochondrial Toxicity Compound Library

Ion Channel Compound Library

Multi-Target Compound Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Clinical Compound Library Plus

Bioactive Compound Library

Protein Kinase Compound Library

High-Throughput Bioactive Compound Library

Mass Spectrometry Human Metabolite Library

Lactylation Compound Library

GPCR/G Protein Compound Library

Membrane Transporter/Ion Channel Compound Library

Neuronal Signaling Compound Library

Protein Tyrosine Kinase Compound Library

Anti-Cancer Compound Library

Clinical Compound Library

Anti-Aging Compound Library

Publications Citing Use of MedChemExpress (MCE) BCTC

All TRP Channel Isoforms

Biological Activity

Chemical Information

Publications (5)

Solvent & Solubility

Purity & Documentation

References

Help & FAQs

Complete Stock Solution Preparation Table

BCTC

Anti-diabetic Compound Library

Orally Active Compound Library

Mechanoreceptors Compound Library

Human Metabolite Library

Pain-Related Compound Library

Metabolic Enzyme Compound Library

Membrane Protein-targeted Compound Library

Membrane Receptor-targeted Compound Library

Mitochondrial Toxicity Compound Library

Ion Channel Compound Library

Multi-Target Compound Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Clinical Compound Library Plus

Bioactive Compound Library

Protein Kinase Compound Library

High-Throughput Bioactive Compound Library

Mass Spectrometry Human Metabolite Library

Lactylation Compound Library

GPCR/G Protein Compound Library

Membrane Transporter/Ion Channel Compound Library

Neuronal Signaling Compound Library

Protein Tyrosine Kinase Compound Library

Anti-Cancer Compound Library

Clinical Compound Library

Anti-Aging Compound Library

Publications Citing Use of MedChemExpress (MCE) BCTC

All TRP Channel Isoforms

Biological Activity

Chemical Information

Publications (5)

Solvent & Solubility

Purity & Documentation

References

Help & FAQs

Complete Stock Solution Preparation Table

BCTC Related Classifications

HY-19960 Related Classifications