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Maprotiline is a highly selective noradrenergic reuptake blocker, has strong antidepressant efficacy. Maprotiline induces cancer cells apoptosis by targeting ERK signaling pathway and CRABP1. Maprotiline restrains cell proliferation and metastasis, exhibits anticancer effect.

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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 blocker, has strong antidepressant efficacy. Maprotiline induces cancer cells apoptosis by targeting ERK signaling pathway and CRABP1. Maprotiline restrains cell proliferation and metastasis, exhibits anticancer effect[1][2].

In Vitro

Maprotiline (10 μM) enhances the sensitivity of HCC cells to sorafenib (2 μM) and induces apoptosis[2].
Maprotiline (0, 10, or 20 μM for 72 h) works on ERK pathway and inhibits phosphorylation of SREBP2 in HepG2 and Huh7 cells[2].
Maprotiline may target CRABP1 and regulate cholesterol biosynthesis in HCC cells[2].

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

Cell Invasion Assay[2]

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[2]

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[2]

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 (3, 10, or 30 mg/kg; i.p.) combinds with the synthetic cannabinoid WIN 55,212-2 and effectively reduces neuropathic pain[1].
Maprotiline (0, 20, or 40 mg/kg; i.p.; twice a week; 3 weeks) shows low toxicity and side effects on the organs, immune system and hematopoietic function[2].
Maprotiline (0, 20, or 40 mg/kg; i.p.; twice a week; 3 weeks) restrains cholesterol biosynthesis to inhibit growth and metastasis of HCC cells by interacting with CRABP1[2].

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

Animal Model: Male Balb-c mice (25–30 g)[1]
Dosage: 3, 10, 30 mg/kg
Administration: Intraperitoneal injection; evaluation 30 minutes after treatment
Result: Attenuated pain-related behaviours in neuropathic mice.
Animal Model: Nude mice (BALB/C nu/nu, 4–6 weeks old, female)[2]
Dosage: 40 mg/kg
Administration: Intraperitoneal injection; 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.
Clinical Trial
Molecular Weight

277.40

Formula

C20H23N

CAS No.
SMILES

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

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Purity & Documentation
References
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    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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