Heptamidine,94345-47-8

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Heptamidine

CAS No. : 94345-47-8

MCE 国际站：Heptamidine

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

研究领域：Others

作用靶点：Others

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.

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.

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