Description
Heptamidine dimethanesulfonate (SBi4211 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).
Product information
CAS Number: 161374-55-6
Molecular Weight: 560.68
Formula: C23H36N4O8S2
Chemical Name: 4-{[7-(4-carbamimidoylphenoxy)heptyl]oxy}benzene-1-carboximidamide; bis(methanesulfonic acid)
Smiles: CS(O)(=O)=O.CS(O)(=O)=O.NC(=N)C1C=CC(=CC=1)OCCCCCCCOC1C=CC(=CC=1)C(N)=N
InChiKey: VJPVVWMWVOBCIC-UHFFFAOYSA-N
InChi: InChI=1S/C21H28N4O2.2CH4O3S/c22-20(23)16-6-10-18(11-7-16)26-14-4-2-1-3-5-15-27-19-12-8-17(9-13-19)21(24)25;2*1-5(2,3)4/h6-13H,1-5,14-15H2,(H3,22,23)(H3,24,25);2*1H3,(H,2,3,4)
Technical Data
Appearance: Solid Power
Purity: ≥98% (or refer to the Certificate of Analysis)
Solubility: DMSO : 62.5 mg/mL (111.47 mM; Need ultrasonic).
Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis
Storage Condition: Dry, dark and -20 oC for 1 year or refer to the Certificate of Analysis.
Shelf Life: ≥12 months if stored properly.
Stock Solution Storage: 0 - 4 oC for 1 month or refer to the Certificate of Analysis.
Drug Formulation: To be determined
HS Tariff Code: 382200
How to use
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.
Products are for research use only. Not for human use.
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