Heptamidine(Synonyms: SBi4211)

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Heptamidine (Synonyms: SBi4211)

Heptamidine (SBi4211) 是一种强效的 Pentamidine-related 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 是研究强直性肌营养不良 (DM) 的有效工具。

Heptamidine(Synonyms: SBi4211)

Heptamidine Chemical Structure

CAS No. : 94345-47-8

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5 mg ￥3000 询问价格 & 货期
10 mg ￥4800 询问价格 & 货期
50 mg ￥13000 询问价格 & 货期
100 mg ￥20000 询问价格 & 货期

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Heptamidine 的其他形式现货产品:

Heptamidine dimethanesulfonate

生物活性

Heptamidine (SBi4211) 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[1]. Heptamidine is a useful tool for the investigation of Myotonic dystrophy (DM)[2].

IC50 & Target

Kd: 6.9 μM (calcium-binding protein S100B)[1]
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[1].
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[2].
Heptamidine rescues mis-splicing of minigene reporters in a HeLa cell DM1 model with an EC50 value of 15 μM[2].

Shanghai Jinpan Biotech Co Ltd 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[2].

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Homozygous HSALR transgenic mice in line 20b (FVB inbred background) with a Myotonic dystrophy (DM) mouse model[2]
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.

分子量

368.47

Formula

C21H28N4O2
CAS 号

94345-47-8
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.
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.

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