化合物 T11553L T11553L

Product Introduction
Bioactivity


英文名: Heptamidine

描述: Heptamidine is an effective Pentamidine-related inhibitor of the calcium-binding protein S100B (Kd: 6.9 μM). It selectively kills melanoma cells with S100B over those without S100B. It is a useful tool for the investigation of Myotonic dystrophy.

体外活性: Heptamidine is a Pentamidine-S100B complex, two molecules of pentamidine bind per monomer of S100B, which is used to be an inhibitor for S100B[1]. Heptamidine rescues mis-splicing of minigene reporters in a HeLa cell DM1 model (EC50 value of 15 μM). When compares to Propamidine and Pentamidine, Heptamidine (20 μM) does not reduce CUG levels?obviously. It shows cytotoxic at concentrations above 17.5 μM in HeLa cells expressing 960 CUG repeats[2].

体内活性: Heptamidine (intraperitoneal injection; 20 or 30 mg/kg; 7 days) induces a dose-dependent reduction of exon 7a inclusion in?HSALR?mice. When at 20 mg/kg dose, returning to wild type levels (6±1%), the myotonia is reduced from grade 3 to grade 1 (occasional myotonic discharge) or grade 0 at both 20 or 30 mg/kg[2].

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

关键字: Heptamidine

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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