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  3. Maprotiline

Maprotiline  (Synonyms: 马普替林)

目录号: HY-B0444A
产品使用指南 技术支持

Maprotiline 是一种高选择性去甲肾上腺素再摄取 (noradrenergic reuptake) 阻滞剂,具有较强的抗抑郁,抗肿瘤和减轻神经性疼痛作用。Maprotiline 通过靶向 ERK 信号通路和 CRABP1 诱导癌细胞凋亡 (apoptosis)。

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Maprotiline Chemical Structure

Maprotiline Chemical Structure

CAS No. : 10262-69-8

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  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

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].

细胞效力
(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]
体外研究
(In Vitro)

Maprotiline (0-20 μM,0-72 h) 抑制 Huh7 和 HepG2 细胞生长并诱导细胞凋亡[1]
Maprotiline (0-20 μM,0-72 h) 抑制肝癌细胞转移[1]
Maprotiline (0-20 μM,72 h) 作用于 ERK 通路并抑制 HepG2 和 Huh7 细胞中 SREBP2 的磷酸化[1]
Maprotiline 靶向 CRABP1 并调节 HCC 细胞中的胆固醇生物合成[1]

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.
体内研究
(In Vivo)

Maprotiline (20-40 mg/kg,腹腔注射,每周两次,三周) 在小鼠中抑制肝癌肿瘤生长[1]
Maprotiline (3-30 mg/kg,静脉注射,单次剂量) 与合成大麻素 WIN 55,212-2 结合,有效减轻小鼠神经性疼痛[2]

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
分子量

277.40

Formula

C20H23N

CAS 号
中文名称

马普替林

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

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

纯度 & 产品资料
参考文献
  • 摩尔计算器

  • 稀释计算器

The molarity calculator equation

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

质量   浓度   体积   分子量 *
= × ×

The dilution calculator equation

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

This equation is commonly abbreviated as: C1V1 = C2V2

浓度 (start) × 体积 (start) = 浓度 (final) × 体积 (final)
× = ×
C1   V1   C2   V2
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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