2. Membrane Transporter/Ion Channel Neuronal Signaling Protein Tyrosine Kinase/RTK GPCR/G Protein
  3. TRP Channel Insulin Receptor CGRP Receptor
  4. BCTC

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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BCTC Chemical Structure

BCTC Chemical Structure

CAS No. : 393514-24-4

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10 mM * 1 mL in DMSO
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Based on 3 publication(s) in Google Scholar

BCTC Related Antibodies

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  • Biological Activity

  • Purity & Documentation

  • References

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Description

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[1][2][3][4][5].

IC50 & Target

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

BCTC Related Antibodies

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.
Molecular Weight

372.89

Formula

C20H25ClN4O
CAS No.
Appearance

Solid

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
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.

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.6818 mL 13.4088 mL 26.8176 mL
5 mM 0.5364 mL 2.6818 mL 5.3635 mL
View the 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.

  • Molarity Calculator

  • Dilution Calculator

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

Mass
=
Concentration
×
Volume
×
Molecular Weight *

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

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

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.

  • 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.

    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.
  • 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

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO +
% 
+
%
Tween-80 +
%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
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.
Purity & Documentation

Purity: 98.03%

COA (247 KB) RP-HPLC (242 KB)

Handling Instructions (2659 KB)
References

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
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BCTC Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

BCTC393514-24-4TRP ChannelInsulin ReceptorCGRP ReceptorTransient receptor potential channelsCalcitonin gene-related peptide receptorNeuropathic painInflammatory painAnalgesiaProstate Cancer (PCa)Type 2 diabetesDU145Inhibitorinhibitorinhibit

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