1. Autophagy Apoptosis Stem Cell/Wnt MAPK/ERK Pathway
  2. Autophagy Apoptosis ERK
  3. Maprotiline hydrochloride

Maprotiline hydrochloride is a highly selective noradrenergic reuptake inhibitor that has strong antidepressant, antitumor and neuropathic pain-relieving effects with oral activity. Maprotiline hydrochloride induces cancer cell apoptosis by targeting the ERK signaling pathway and CRABP1.

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Maprotiline hydrochloride Chemical Structure

Maprotiline hydrochloride Chemical Structure

CAS No. : 10347-81-6

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Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
USD 73 In-stock
Solution
10 mM * 1 mL in DMSO USD 73 In-stock
Solid
100 mg USD 66 In-stock
500 mg USD 132 In-stock
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Based on 2 publication(s) in Google Scholar

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  • References

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Description

Maprotiline hydrochloride is a highly selective noradrenergic reuptake inhibitor that has strong antidepressant, antitumor and neuropathic pain-relieving effects with oral activity. Maprotiline hydrochloride induces cancer cell apoptosis by targeting the ERK signaling pathway and CRABP1[1][2].

In Vitro

Maprotiline (0-20 μM, 0-72 h) hydrochloride inhibits the growth of Huh7 and HepG2 cells and induces cell apoptosis[1].
Maprotiline (0-20 μM, 0-72 h) hydrochloride inhibits the metastasis of liver cancer cells[1].
Maprotiline (0-20 μM, 72 h) hydrochloride affects the ERK pathway and inhibits the phosphorylation of SREBP2 in HepG2 and Huh7 cells[1].
Maprotiline hydrochloride targets CRABP1 and regulates cholesterol biosynthesis in HCC cells[1].

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

Cell Invasion Assay[1]

Cell Line: The human HCC cell lines Huh7 and HepG2
Concentration: 0, 10, 20 μM
Incubation Time: 24 h
Result: Restrained HCC cells migration with inhibition of epithelial-mesenchymal transition (EMT).

Cell Viability Assay[1]

Cell Line: The human HCC cell lines Huh7 and HepG2
Concentration: 0, 10, 20 μM
Incubation Time: 0, 24, 48, 72, 96, 120 h
Result: Triggered cell apoptosis and inhibited the cell viability of Huh7 and HepG2 cells in a dose- and time-dependent manner.

Western Blot Analysis[1]

Cell Line: The human HCC cell lines Huh7 and HepG2
Concentration: 0, 10, 20 μM
Incubation Time: 72 h
Result: Inhibited cholesterol biosynthesis in HCC Cells.
In Vivo

Maprotiline (20-40 mg/kg, intraperitoneal injection, twice a week for three weeks) hydrochloride inhibits liver cancer tumor growth in mice[1].
Maprotiline (3-30 mg/kg, intravenous injection, single dose) hydrochloride combined with the synthetic cannabinoid WIN 55,212-2 effectively reduces neuropathic pain in mice[2].

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

Animal Model: Nude mice (BALB/C nu/nu, 4–6 weeks old, female)[1]
Dosage: 20, 40 mg/kg
Administration: Intraperitoneal injection (i.p.); twice a week; 3 weeks
Result: Decreased the cholesterol levels in serum and tumors and suppressed the growth of Huh7-derived tumor xenografts without obvious toxic effect.
Animal Model: Male Balb-c mice (25–30 g)[2]
Dosage: 3, 10, 30 mg/kg; single dose
Administration: Intravenous injection (i.v.)
Result: Attenuated pain-related behaviours in neuropathic mice.
Clinical Trial
Molecular Weight

313.86

Formula

C20H24ClN

CAS No.
Appearance

Solid

Color

White to off-white

SMILES

CNCCCC1(CC2)C3=CC=CC=C3C2C4=CC=CC=C14.Cl

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

4°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

Solvent & Solubility
In Vitro: 

DMSO : 83.33 mg/mL (265.50 mM; ultrasonic and warming and heat to 60°C; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

H2O : 2.2 mg/mL (7.01 mM; Need ultrasonic)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 3.1861 mL 15.9307 mL 31.8613 mL
5 mM 0.6372 mL 3.1861 mL 6.3723 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, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

  • Molarity Calculator

  • Dilution Calculator

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

Mass
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Concentration
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Volume
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Molecular Weight *

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

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

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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    40% PEG300    5% Tween-80    45% Saline

    Solubility: ≥ 2.08 mg/mL (6.63 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

    Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
  • Protocol 2

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

    Solubility: ≥ 2.08 mg/mL (6.63 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 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.

For the following dissolution methods, please prepare the working solution directly. It is recommended to prepare fresh solutions and use them promptly within a short period of time.
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:  PBS

    Solubility: 2 mg/mL (6.37 mM); Clear solution; Need ultrasonic and warming and heat to 60°C

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).

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

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: 99.98%

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, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
H2O / DMSO 1 mM 3.1861 mL 15.9307 mL 31.8613 mL 79.6534 mL
5 mM 0.6372 mL 3.1861 mL 6.3723 mL 15.9307 mL
DMSO 10 mM 0.3186 mL 1.5931 mL 3.1861 mL 7.9653 mL
15 mM 0.2124 mL 1.0620 mL 2.1241 mL 5.3102 mL
20 mM 0.1593 mL 0.7965 mL 1.5931 mL 3.9827 mL
25 mM 0.1274 mL 0.6372 mL 1.2745 mL 3.1861 mL
30 mM 0.1062 mL 0.5310 mL 1.0620 mL 2.6551 mL
40 mM 0.0797 mL 0.3983 mL 0.7965 mL 1.9913 mL
50 mM 0.0637 mL 0.3186 mL 0.6372 mL 1.5931 mL
60 mM 0.0531 mL 0.2655 mL 0.5310 mL 1.3276 mL
80 mM 0.0398 mL 0.1991 mL 0.3983 mL 0.9957 mL
100 mM 0.0319 mL 0.1593 mL 0.3186 mL 0.7965 mL

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

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Maprotiline hydrochloride
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