Heptamidine dimethanesulfonate

SKU: orb1309580

Description

Heptamidine dimethanesulfonate is a potent S100B inhibitor (Kd 6.9 µM) derived from Pentamidine, showing selective cytotoxicity against S100B-overexpressing melanoma cells. It is also utilized as a research tool in studies of Myotonic Dystrophy (DM), applicable in both in vitro and in vivo experimental models.

Key Properties

• CAS Number: 161374-55-6
• MW: 560.68
• Purity: 98.24% (May vary between batches)
• Formula: C₂₃H₃₆N₄O₈S₂
• SMILES: CS(O)(=O)=O.CS(O)(=O)=O.NC(=N)c1ccc(OCCCCCCCOc2ccc(cc2)C(N)=N)cc1
• Target: Others
• Solubility: H2O:8.33 mg/mL (14.86 mM);10% DMSO+40% PEG300+5% Tween 80+45% Saline:2 mg/mL (3.57 mM);DMSO:70 mg/mL (124.85 mM)

Bioactivity

• Target IC50:
  S100B:(kd)6.9 μM
• In Vivo:
  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 .
• In Vitro:
  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 .

Storage & Handling

• Storage: Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

cell, dystrophy, cancer, Calcium-Binding, calcium-binding protein S100B, inhibit, Myotonic, Inhibitor, Heptamidine, Heptamidine dimethanesulfonate, HeLa, melanoma, S100B, SBi4211, SBi-4211, SBi4211 dimethanesulfonate, SBi 4211

Compound Identifiers

PubChem CID

146047121