BCTC
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.
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- Pureza : 99.66%
- No. CAS: 393514-24-4
- Fòrmula: C20H25ClN4O
- Peso molecular:372.89
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Almacenamiento:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
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Actividad biológica
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Chemical Information
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Solvente y solubilidad
- Protocolo
- Pureza y Documentación
- Referencias
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Publications Citing Use of MedChemExpress (MCE) BCTC
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Actividad biológica
Descripciòn
IC50 & Target
Cellular Effect
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| CHO | IC50 |
0.4 nM
Compound: 4
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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
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[PMID: 16759115] |
| CHO | IC50 |
0.5 nM
Compound: 5
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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
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[PMID: 17489570] |
| CHO | IC50 |
0.5 nM
Compound: 4
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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
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[PMID: 16759115] |
| CHO | IC50 |
0.6 nM
Compound: 5
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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
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[PMID: 17489570] |
| CHO | IC50 |
0.7 nM
Compound: 5
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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
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[PMID: 17489570] |
| CHO | IC50 |
0.7 nM
Compound: 5
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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
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[PMID: 17489570] |
| CHO-K1 | IC50 |
0.019 μM
Compound: BCTC
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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
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[PMID: 31202991] |
| HEK293 | EC50 |
4.5 μM
Compound: BCTC
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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
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[PMID: 19875281] |
| HEK293 | IC50 |
0.0067 μM
Compound: BCTC
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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
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[PMID: 19875281] |
| HEK293 | IC50 |
0.6 nM
Compound: 5
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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
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[PMID: 17489570] |
| HEK293 | IC50 |
0.6 nM
Compound: 5
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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
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[PMID: 17489570] |
| HEK293 | IC50 |
1.9 nM
Compound: 5
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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
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[PMID: 17489570] |
| HEK293 | IC50 |
29.8 nM
Compound: BCTC
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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
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[PMID: 15482915] |
| HEK293 | IC50 |
34 nM
Compound: BCTC
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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
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[PMID: 15482915] |
| HEK293 | IC50 |
34.9 nM
Compound: 18
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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
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[PMID: 14505681] |
| HEK293 | IC50 |
4.8 nM
Compound: 18
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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
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[PMID: 14505681] |
| HEK293 | IC50 |
475 nM
Compound: BCTC
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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
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[PMID: 26847872] |
| HEK293 | IC50 |
5 nM
Compound: 5
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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
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[PMID: 17489570] |
| HEK-293T | IC50 |
0.15 nM
Compound: BCTC
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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
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[PMID: 24484240] |
| HEK-293T | IC50 |
2.12 nM
Compound: BCTC
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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
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[PMID: 23796768] |
| HEK-293T | IC50 |
4.86 nM
Compound: BCTC
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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
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[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. Further protocols information, click here.
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Cell Line:DU145
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Concentration:20 μM, 40 μM, 60 μM, 80 μM,100 μM
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Incubation Time:48 h
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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.
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Cell Line:DU145, PNT1A
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Concentration:20 μM, 40 μM, 60 μM, 80 μM,100 μM
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Incubation Time:72 h
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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 (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.
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Animal Model:Capsaicin-induced Sprague-Dawley rats model[2]
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Dosage:1 mg/kg, 3 mg/kg, 10 mg/kg, 30 mg/kg
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Administration:Oral gavage (p.o.), Single dose. Before capsaicin (HY-10448) treatment (30 μg; intraplantar injection; Single dose)
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Result:Inhibited capsaicin-mediated thermal hyperalgesia in a dose-dependent manner.
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Animal Model:Freund’s complete adjuvant (FCA) Sprague-Dawley rats model[2]
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Dosage:1 mg/kg, 3 mg/kg, 10 mg/kg, 30 mg/kg
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Administration:Oral gavage (p.o.), Single dose. After 100 % FAC treatment (50 μL; intraplantar injection; Single dose)
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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).
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Animal Model:Partial sciatic nerve ligation Sprague-Dawley rats model[2]
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Dosage:1 mg/kg, 3 mg/kg, 10 mg/kg, 30 mg/kg
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Administration:Oral gavage (p.o.), Single dose. After partial sciatic nerve ligation.
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Result:Reduced post-operative abnormal tactile pain and mechanical hyperalgesia in a dose-dependent manner.
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Animal Model:Particularly strong insulin resistance and hyperinsulinemia ob/ob mice model[5]
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Dosage:10 mg/kg, 30 mg/kg, 100 mg/kg
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Administration:Oral gavage (p.o.); Twice daily for 4 weeks
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Result:Reduced plasma triglyceride and glucose area under the curve (AUC) level.
Decreased calcitonin gene-related peptide (CGRP) levels in a dose-dependent manner.
Ensayo clínico
| NCT Number | Sponsor | Condition | Start Date |
Phase
|
|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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No. CAS 393514-24-4
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Appearance Solid
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Peso molecular 372.89
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Fòrmula C20H25ClN4O
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Color White to off-white
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SMILES
O=C(N1CCN(C2=NC=CC=C2Cl)CC1)NC3=CC=C(C(C)(C)C)C=C3
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
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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Journal Impact Factor
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Most Recent
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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
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 -
Solvente y solubilidad
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.
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.
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.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
In Vivo:
Select the appropriate dissolution method based on your experimental animal and administration route.
- 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.
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.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%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
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Protocolo
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Research Protocol for Endocrine Diseases
Endocrine diseases often arise from disrupted hormone production, hormone signaling, or target-tissue responsiveness; for diabetes-focused endocrine disease models, insulin signaling regulates glucose uptake, hepatic glucose output, lipid metabolism, and β-cell compensation. Type 2 diabetes develops through interacting defects in insulin resistance, β-cell dysfunction, adipose inflammation, hepatic glucose overproduction, altered incretin signaling, and ectopic lipid metabolism. A major unresolved question is whether endocrine dysfunction is driven primarily by target-tissue insulin resistance, intrinsic β-cell failure, immune/inflammatory stress, or combined multi-organ failure that differs by disease stage.
Pureza y Documentación
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Ficha de datos (282 KB)
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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)
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Instrucciones de manejo (2659 KB)
Referencias
[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]
Complete Stock Solution Preparation Table
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.
| 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 |
BCTC Related Classifications
HY-19960 Related Classifications
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