Maprotiline 是一种高选择性去甲肾上腺素再摄取 (noradrenergic reuptake) 阻滞剂，具有较强的抗抑郁效果。Maprotiline 通过靶向ERK信号通路和CRABP1诱导癌细胞凋亡 (apoptosis)。马普替林抑制细胞增殖和转移，具有抗癌作用。
| 生物活性 | Maprotiline is a highly selectivenoradrenergic reuptakeblocker, has strongantidepressantefficacy. Maprotiline inducescancercellsapoptosisby targetingERKsignaling pathway andCRABP1. Maprotiline restrains cell proliferation and metastasis, exhibitsanticancereffect[1][2]. |
体外研究
(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].
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. |
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体内研究
(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].
| 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. |
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| 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. |
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