Heptamidine dimethanesulfonate

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

Heptamidine dimethylsulfonate 是钙结合蛋白 S100B 的喷他脒相关抑制剂（Kd：6.9 μM）。

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).

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.

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.

SBi4211 dimethanesulfonate

Others

Other Targets

calcium-binding protein S100B

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161374-55-6

560.68

C23H36N4O8S2

>98% (HPLC)

DMSO:62.5 mg/mL (111.47 mM; Need ultrasonic)

N=C(C1=CC=C(OCCCCCCCOC2=CC=C(C(N)=N)C=C2)C=C1)N.CS(=O)(O)=O.CS(=O)(O)=O

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(-20℃)

With Ice Pack

≥ 2 years