161374-55-6
161374-55-6 structure
- Name: Heptamidine dimethanesulfonate
- Chemical Name: Heptamidine dimethanesulfonate
- CAS Number: 161374-55-6
- Molecular Formula: C23H36N4O8S2
- Molecular Weight: 560.68
- Catalog: Research Areas Inflammation/Immunology
- Create Date: 2020-06-01 23:28:41
- Modify Date: 2024-01-11 22:33:40
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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[1]. Heptamidine is a useful tool for the investigation of Myotonic dystrophy (DM)[2].
| Name | Heptamidine dimethanesulfonate |
|---|
| 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[1]. Heptamidine is a useful tool for the investigation of Myotonic dystrophy (DM)[2]. |
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| Related Catalog | |
| Target |
Kd: 6.9 μM (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 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]. Heptamidine rescues mis-splicing of minigene reporters in a HeLa cell DM1 model with an EC50 value of 15 μM[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]. Animal Model: Homozygous HSALR transgenic mice in line 20b (FVB inbred background) with a Myotonic dystrophy (DM) mouse model[2] 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. |
| References |
| Molecular Formula | C23H36N4O8S2 |
|---|---|
| Molecular Weight | 560.68 |