化合物 Maprotiline T60509

Product Introduction
Bioactivity


英文名: Maprotiline

描述: Maprotiline 能够抑制细胞的增殖和转移，具有抗癌作用。 Maprotiline 通过靶向 ERK 信号通路和 CRABP1 诱导癌细胞凋亡。 Maprotiline 是一种高度选择性的去甲肾上腺素再摄取阻滞剂，具有有效的抗抑郁作用 [1][2]。

体外活性: 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 targets 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.

体内活性: Maprotiline (intraperitoneal injection; 3, 10, or 30 mg/kg) combinds with the synthetic cannabinoid WIN 55,212-2 and effectively reduces neuropathic pain [1]. Maprotiline (intraperitoneal injection; 0, 20, or 40 mg/kg; twice a week; 3 weeks) shows low toxicity and side effects on the organs, immune system and hematopoietic function [2]. Maprotiline (intraperitoneal injection; 0, 20, or 40 mg/kg; 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.

存储条件: Powder: -20°C for 3 years | In solvent: -80°C for 1 year

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注：该产品未在中华人民共和国食品药品监督管理部门申请医疗器械注册和备案，不可用于临床诊断或治疗等相关用途