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  3. Maprotiline

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

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Maprotiline Chemical Structure

Maprotiline Chemical Structure

CAS No. : 10262-69-8

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Description

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

Cellular Effect
Cell Line Type Value Description References
DG-75 EC50
37.5 μM
Compound: 1
Antiproliferative activity against human DG75 cells after 72 hrs by Alamar blue assay
Antiproliferative activity against human DG75 cells after 72 hrs by Alamar blue assay
[PMID: 24333581]
Ventricular myocyte IC50
31 μM
Compound: Maprotiline
Inhibition of L-type calcium channel measured using whole-cell patch clamp in rat ventricular myocytes
Inhibition of L-type calcium channel measured using whole-cell patch clamp in rat ventricular myocytes
[PMID: 22761000]
In Vitro

Maprotiline (0-20 μM, 0-72 h) inhibits the growth of Huh7 and HepG2 cells and induces cell apoptosis[1].
Maprotiline (0-20 μM, 0-72 h) inhibits the metastasis of liver cancer cells[1].
Maprotiline (0-20 μM, 72 h) affects the ERK pathway and inhibits the phosphorylation of SREBP2 in HepG2 and Huh7 cells[1].
Maprotiline 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 hours
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 hours
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 hours
Result: Inhibited cholesterol biosynthesis in HCC Cells.
In Vivo

Maprotiline (20-40 mg/kg, intraperitoneal injection, twice a week for three weeks) inhibits liver cancer tumor growth in mice[1].
Maprotiline (3-30 mg/kg, intravenous injection, single dose) 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

277.40

Formula

C20H23N

CAS No.
SMILES

CNCCCC12C3=C(C=CC=C3)C(CC2)C4=CC=CC=C14

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

Purity & Documentation
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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.

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Maprotiline
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HY-B0444A
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