SBi4211 dimethanesulfonate
Heptamidine dimethanesulfonate
CAS: 161374-55-6
Molecular Formula: C22H32N4O5S
SBi4211 dimethanesulfonate - Names and Identifiers
| Name | Heptamidine dimethanesulfonate |
| Synonyms | SBi4211 dimethanesulfonate Heptamidine dimethanesulfote Heptamidine dimethanesulfonate 4,4'-(Heptane-1,7-diylbis(oxy))dibenzimidamide dimethanesulfonate |
| CAS | 161374-55-6 |
SBi4211 dimethanesulfonate - Physico-chemical Properties
| Molecular Formula | C22H32N4O5S |
| Molar Mass | 464.58 |
| Appearance | Solid |
| Storage Condition | 2-8°C，密封，干燥 |
| In vitro study | 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 levelssignificantly 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 EC 50 value of 15 μM. |
| In vivo study | Heptamidine (intraperitoneal injection; 20 or 30 mg/kg; 7 days) causes a dose-dependent reduction of exon 7a inclusion in HSA LRmice, 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: HomozygousHSALRtransgenic 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. |
SBi4211 dimethanesulfonate - Reference Information
| biological activity | Heptamidine dimethanesulfonate (SBi4211 dimethanesulfonate) is a potent inhibitor of calcium binding protein S100B (Kd = 6.9 μM) related to pentamidine (HY-B0537), which selectively kills melanoma cells expressing S100B. Heptamidine dimethanesulfonate is an effective tool to study myotonic dystrophy (DM). |
| target | Kd: 6.9 μM (calcium-binding protein S100B) |
| in vitro study | 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 μ m) does not decrease CUG levelssignificantly 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 EC 50 value of 15 μM. |
| in vivo research | Heptamidine (intraperitoneal injection; 20 or 30 mg/kg; 7 days) cause a dose-dependent reduction of exon 7a inclusion in HSA LRmice, 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: homozygousHSALRtransgenic 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. |
| Animal Model: | HomozygousHSALRtransgenic 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. |
Last Update：2024-04-09 21:01:54
