Heptamidine dimethanesulfonate

SKU: orb1218699

Description

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).

Key Properties

• CAS Number: 161374-55-6
• MW: 560.68
• Purity: >98% (HPLC)
• Formula: C₂₃H₃₆N₄O₈S₂
• SMILES: N=C(C1=CC=C(OCCCCCCCOC2=CC=C(C(N)=N)C=C2)C=C1)N.CS(=O)(O)=O.CS(=O)(O)=O
• Target: calcium-binding protein S100B
• Solubility: DMSO:62.5 mg/mL (111.47 mM; Need ultrasonic)

Bioactivity

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

Storage & Handling

• Storage: Storage temperature: -20°C. Stability: ≥ 2 years
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

SBi4211 dimethanesulfonate

Quick Database Links

Gene Symbol

calcium-binding protein S100B