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Heptamidine dimethanesulfonate

(Synonyms: SBi4211 dimethanesulfonate)

目录号: PL08613 纯度: ≥99%

Heptamidine dimethanesulfonate (SBi4211 dimethanesulfonate) 是一种强效的，与喷他脒 (HY-B0537) 有关的钙结合蛋白 S100B 的抑制剂 (Kd=6.9 μM)，选择性地杀死表达 S100B 的黑素瘤细胞。Heptamidine dimethanesulfonate 是研究强直性肌营养不良 (DM) 的有效工具。

CAS No. :161374-55-6

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中文名称	Heptamidine dimethanesulfonate
英文名称	Heptamidine dimethanesulfonate
英文别名	Heptamidine (dimethanesulfonate);4,4'-(Heptane-1,7-diylbis(oxy))dibenzimidamide dimethanesulfonate;Heptamidine dimethanesulfonate;SBi4211 dimethanesulfonate
Cas No.	161374-55-6
分子式	C₂₃H₃₆N₄O₈S₂
分子量	560.68
包装储存	4°C, sealed storage, away from moistur In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
详情描述	Heptamidine dimethanesulfonate (SBi4211 dimethanesulfonate) 是一种强效的，与喷他脒 (HY-B0537) 有关的钙结合蛋白 S100B 的抑制剂 (Kd=6.9 μM)，选择性地杀死表达 S100B 的黑素瘤细胞。Heptamidine dimethanesulfonate 是研究强直性肌营养不良 (DM) 的有效工具。

产品详情	Heptamidine dimethanesulfonate (SBi4211 dimethanesulfonate) 是一种强效的，与喷他脒 (HY-B0537) 有关的钙结合蛋白 S100B 的抑制剂 (K_d=6.9 μM)，选择性地杀死表达 S100B 的黑素瘤细胞。Heptamidine dimethanesulfonate 是研究强直性肌营养不良 (DM) 的有效工具。
生物活性	Heptamidine dimethanesulfonate (SBi4211 dimethanesulfonate) is a potent Pentamidine-related inhibitor of the calcium-binding protein S100B (K d =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).
性状	Solid
IC50 & Target[1][2]	Kd: 6.9 μM (calcium-binding protein S100B)
体外研究(In Vitro)	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. has not independently confirmed the accuracy of these methods. They are for reference only.
体内研究(In Vivo)	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. has not independently confirmed the accuracy of these methods. They are for reference only.
运输条件	Room temperature in continental US; may vary elsewhere.
储存方式	4°C, sealed storage, away from moistur In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
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.

溶解度数据	In Vitro: DMSO : 62.5 mg/mL (111.47 mM; Need ultrasonic)配制储备液

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[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.

1：一般建议：溶解度为Medlife测试数据，可能与文献描述存在差异。这是由于生产工艺和批次不同产生的正常现象。为了使其更好的溶解，请用37℃加热试管并在超声波水浴中震动片刻。不同批次产品溶解度各有差异，仅做参考，具体以实验方案为准。

2：储存条件：粉末-20°C一般情况可以保存3年，溶于溶剂-80°C一般情况可以保存1年。不同产品及不同批次产品可能存在差异，请细致阅读产品信息，并辅助参考相关文献描述。

Heptamidine dimethanesulfonate

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