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二甲基磺酸庚胺

    
10mM in DMSO

SBi4211 dimethanesulfonate

源叶(MedMol)
V54141 一键复制产品信息
161374-55-6
C23H36N4O8S2
560.68
SBi4211 dimethanesulfonate
货号 规格 价格 上海 北京 珠海 重庆 武汉 购买数量
V54141-1ml
10mM in DMSO

¥1790.00

货期:3-5天 - - - -
产品介绍 参考文献 质检证书(COA) 摩尔浓度计算器 相关产品
产品描述: Heptamidine dimethanesulfonate (SBi4211 dimethanesulfonate) is a potent Pentamidine-related inhibitor of the calcium-binding protein S100B (Kd=6.9 μM), selectively kills melanoma cells with S100B over those without S100B. Heptamidine is a useful tool for the investigation of Myotonic dystrophy (DM)
靶点: Kd: 6.9 μM (calcium-binding protein S100B)
体外研究: Heptamidine is a Pentamidine-S100B complex, two molecules of pentamidine bind per monomer of S100B, which performs to be an inhibitor for S100B.

Heptamidine (20 μM) does not decrease CUG levels significantly when compares to Propamidine and Pentamidine, and exhibits cytotoxic at concentrations above 17.5 μM in HeLa cells expressing 960 CUG repeats.
Heptamidine rescues mis-splicing of minigene reporters in a HeLa cell DM1 model with an EC50 value of 15 μM[2].
体内研究: Heptamidine (intraperitoneal injection; 20 or 30 mg/kg; 7 days) causes a dose-dependent reduction of exon 7a inclusion in HSALR mice, returning to wild type levels (6±1%) when at 20 mg/kg dose, the myotonia is reduced from grade 3 to grade 1 (occasional myotonic discharge) or grade 0 at both 20 or 30 mg/kg. Animal Model: Homozygous HSALR transgenic mice in line 20b (FVB inbred background) with a Myotonic dystrophy (DM) mouse model Dosage: 20 or 30 mg/kg Administration: Intraperitoneal injection; 7 days; once daily Result: Reversed splicing defects and rescues myotonia in a DM mouse model.
参考文献: 1. McKnight LE, et al. Structure-Based Discovery of a Novel Pentamidine-Related Inhibitor of the Calcium-Binding Protein S100B. ACS Med Chem Lett. 2012 Dec 13;3(12):975-979. Epub 2012 Sep 25.

2. Coonrod LA, et al. Reducing levels of toxic RNA with small molecules.ACS Chem Biol. 2013 Nov 15;8(11):2528-37.
溶解性: Soluble  in  DMSO
保存条件: -80℃(运输条件:冰袋低温运输)
配置溶液浓度参考:
1mg 5mg 10mg
1 mM 1.784 ml 8.918 ml 17.835 ml
5 mM 0.357 ml 1.784 ml 3.567 ml
10 mM 0.178 ml 0.892 ml 1.784 ml
50 mM 0.036 ml 0.178 ml 0.357 ml
注意: 部分产品我司仅能提供部分信息,我司不保证所提供信息的权威性,仅供客户参考交流研究之用。

参考文献

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摩尔浓度计算器

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