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Heptamidine dimethanesulfonate (SBi4211 dimethanesulfonate) serves as a potent inhibitor related to Pentamidine, targeting the calcium-binding protein S100B with a dissociation constant (Kd) of 6.9 µM. It demonstrates specificity by preferentially killing melanoma cells overexpressing S100B compared to cells lacking this protein. Additionally, Heptamidine is employed as a valuable research tool in the study of Myotonic dystrophy (DM).
Pack Size | Price | Availability | Quantity |
---|---|---|---|
1 mg | $74 | In Stock | |
5 mg | $179 | In Stock | |
10 mg | $289 | In Stock | |
25 mg | $496 | In Stock | |
50 mg | $745 | In Stock | |
100 mg | $1,090 | In Stock | |
1 mL x 10 mM (in DMSO) | $223 | In Stock |
Description | Heptamidine dimethanesulfonate (SBi4211 dimethanesulfonate) serves as a potent inhibitor related to Pentamidine, targeting the calcium-binding protein S100B with a dissociation constant (Kd) of 6.9 µM. It demonstrates specificity by preferentially killing melanoma cells overexpressing S100B compared to cells lacking this protein. Additionally, Heptamidine is employed as a valuable research tool in the study of Myotonic dystrophy (DM). |
Targets&IC50 | S100B:(kd)6.9 μM |
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 [2]. |
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 [2]. |
Alias | SBi4211 dimethanesulfonate |
Molecular Weight | 560.68 |
Formula | C23H36N4O8S2 |
Cas No. | 161374-55-6 |
Smiles | CS(O)(=O)=O.CS(O)(=O)=O.NC(=N)c1ccc(OCCCCCCCOc2ccc(cc2)C(N)=N)cc1 |
Relative Density. | no data available |
Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. | ||||||||||||||||||||||||||||||||||||||||
Solubility Information | H2O: 8.33 mg/mL (14.86 mM), Sonication is recommended. DMSO: 70 mg/mL (124.85 mM), Sonication is recommended. | ||||||||||||||||||||||||||||||||||||||||
Solution Preparation Table | |||||||||||||||||||||||||||||||||||||||||
H2O/DMSO
DMSO
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