Heptamidine dimethanesulfonate 是一种与喷他脒有关的、强效的钙结合蛋白S100B的抑制剂 (Kd=6.9 μM)，选择性地杀死表达 S100B 的黑素瘤细胞。它是有效的强直性肌营养不良 (DM) 研究工具。

Heptamidine 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).

Heptamidine rescues the mis-splicing of minigene reporters in a HeLa cell DM1 model (EC50: 15 μM). 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 (i.p.; 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].

161374-55-6

C22H32N4O5S

464.58

SBi4211 dimethanesulfonate

DMSO:62.5 mg/mL (111.47 mM),Need ultrasonic
Powder: -20°C for 3 years
In solvent: -80°C for 2 years