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Heptamidine dimethanesulfonateCAS No. : 161374-55-6
MCE 國際站:Heptamidine dimethanesulfonate
產品活性:Heptamidine dimethanesulfonate (SBi4211 dimethanesulfonate) 是一種強效的,與噴他脒 (HY-B0537) 有關的鈣結合蛋白 S100B 的抑制劑 (Kd=6.9 μM),選擇性地殺死表達 S100B 的黑素瘤細胞。Heptamidine dimethanesulfonate 是研究強直性肌營養(yǎng)不良 (DM) 的有效工具。
研究領域:Others
作用靶點:Others
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.
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