Maprotiline hydrochloride
Based on 4 publication(s) in Google Scholar
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.
For research use only. We do not sell to patients.
- Purity: 99.84%
- CAS No.: 10347-81-6
- Formula: C20H24ClN
- Molecular Weight:313.86
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Storage:
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
Publications Citing Use of MedChemExpress (MCE) Maprotiline hydrochloride
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Biological Activity
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| HEK293 | IC50 |
0.05 μM
Compound: Maprotiline
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Inhibition of the Norepinephrine transporter (NET, SLC6A2) as assessed by GPCR-mediated changes in cell morphology using the impedance-based transporter activity through receptor activation (TRACT) assay in HEK-293 JumpIN-SLC6A2 cells (PubChem AID: 174586
Inhibition of the Norepinephrine transporter (NET, SLC6A2) as assessed by GPCR-mediated changes in cell morphology using the impedance-based transporter activity through receptor activation (TRACT) assay in HEK-293 JumpIN-SLC6A2 cells (PubChem AID: 174586
|
[PMID: 34112854] |
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.
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Cell Line:The human HCC cell lines Huh7 and HepG2
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Concentration:0, 10, 20 μM
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Incubation Time:24 h
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Result:Restrained HCC cells migration with inhibition of epithelial-mesenchymal transition (EMT).
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Cell Line:The human HCC cell lines Huh7 and HepG2
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Concentration:0, 10, 20 μM
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Incubation Time:0, 24, 48, 72, 96, 120 h
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Result:Triggered cell apoptosis and inhibited the cell viability of Huh7 and HepG2 cells in a dose- and time-dependent manner.
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Cell Line:The human HCC cell lines Huh7 and HepG2
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Concentration:0, 10, 20 μM
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Incubation Time:72 h
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Result:Inhibited cholesterol biosynthesis in HCC Cells.
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.
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Animal Model:Nude mice (BALB/C nu/nu, 4–6 weeks old, female)[1]
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Dosage:20, 40 mg/kg
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Administration:Intraperitoneal injection (i.p.); twice a week; 3 weeks
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Result:Decreased the cholesterol levels in serum and tumors and suppressed the growth of Huh7-derived tumor xenografts without obvious toxic effect.
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Animal Model:Male Balb-c mice (25–30 g)[2]
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Dosage:3, 10, 30 mg/kg; single dose
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Administration:Intravenous injection (i.v.)
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Result:Attenuated pain-related behaviours in neuropathic mice.
| NCT Number | Sponsor | Condition | Start Date |
Phase
|
|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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CAS No. 10347-81-6
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Appearance Solid
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Molecular Weight 313.86
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Formula C20H24ClN
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Color White to off-white
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SMILES
CNCCCC1(CC2)C3=CC=CC=C3C2C4=CC=CC=C14.Cl
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
Publications (4)
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Journal Impact Factor
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Most Recent
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Autophagy
2025 May;21(5):934-956. PMID: 39663580 -
Adv Sci (Weinh)
Network Medicine-Based Strategy Identifies Maprotiline as a Repurposable Drug by Inhibiting PD-L1 Expression via Targeting SPOP in Cancer. [Abstract]2025 Jan;12(1):e2410285. PMID: 39499771 -
Cell Rep Methods
RECOVER identifies synergistic drug combinations in vitro through sequential model optimization. [Abstract]2023 Oct 23;3(10):100599. PMID: 37797618 -
PLoS Negl Trop Dis
Identification of anti-flaviviral drugs with mosquitocidal and anti-Zika virus activity in Aedes aegypti. [Abstract]2019 Aug 20;13(8):e0007681. PMID: 31430351
Solvent & Solubility
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)
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.
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.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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 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.
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.
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
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. * In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
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.
Purity & Documentation
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Data Sheet (283 KB)
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SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
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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, 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.