Heptamidine (dimethanesulfonate)

161374-55-6

560.68

DMSO : 62.5 mg/mL (111.47 mM; Need ultrasonic)

Others

Heptamidine dimethanesulfonate (SBi4211 dimethanesulfonate) is a potent Pentamidine-related inhibitor of the calcium-binding protein S100B (K_d=6.9 uM), 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 uM (calcium-binding protein S100B)^[1] 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 uM) does not decrease CUG levels significantly when compares to Propamidine and Pentamidine, and exhibits cytotoxic at concentrations above 17.5 uM 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 uM^[2].
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].