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Heptamidine dimethanesulfonate (SBi4211 dimethanesulfonate) 是一种与喷他脒有关的、强效的钙结合蛋白 S100B 的抑制剂 (Kd=6.9 μM),选择性地杀死表达 S100B 的黑素瘤细胞。它是有效的强直性肌营养不良 (DM) 研究工具。
Heptamidine dimethanesulfonate (SBi4211 dimethanesulfonate) 是一种与喷他脒有关的、强效的钙结合蛋白 S100B 的抑制剂 (Kd=6.9 μM),选择性地杀死表达 S100B 的黑素瘤细胞。它是有效的强直性肌营养不良 (DM) 研究工具。
规格 | 价格 | 库存 | 数量 |
---|---|---|---|
1 mg | ¥ 593 | 现货 | |
5 mg | ¥ 1,450 | 现货 | |
10 mg | ¥ 2,320 | 现货 | |
25 mg | ¥ 3,980 | 现货 | |
50 mg | ¥ 5,970 | 现货 | |
100 mg | ¥ 7,880 | 现货 | |
500 mg | ¥ 15,900 | 现货 | |
1 mL x 10 mM (in DMSO) | ¥ 1,780 | 现货 |
产品描述 | 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). |
靶点活性 | S100B:(kd)6.9 μM |
体外活性 | Heptamidine在HeLa细胞DM1模型中纠正minigene报告基因片段剪接错误(EC50:15 μM)。与Propamidine和Pentamidine相比,Heptamidine(20 μM)并未显著降低CUG水平,且在表达960个CUG重复序列的HeLa细胞中,浓度超过17.5 μM时表现出细胞毒性[2]。 |
体内活性 | Heptamidine(i.p.;20或30 mg/kg;7天)在HSALR小鼠中引起剂量依赖性的exon 7a含量减少,20 mg/kg剂量时回复至野生型水平(6±1%),同时肌阵挛从3级(频繁的肌阵挛放电)降低至1级(偶尔的肌阵挛放电)[2]。 |
别名 | SBi4211 dimethanesulfonate |
分子量 | 560.68 |
分子式 | C23H36N4O8S2 |
CAS No. | 161374-55-6 |
Smiles | CS(O)(=O)=O.CS(O)(=O)=O.NC(=N)c1ccc(OCCCCCCCOc2ccc(cc2)C(N)=N)cc1 |
密度 | no data available |
存储 | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. | ||||||||||||||||||||||||||||||||||||||||
溶解度信息 | H2O: 8.33 mg/mL (14.86 mM), Sonication is recommended. DMSO: 70 mg/mL (124.85 mM), Sonication is recommended. | ||||||||||||||||||||||||||||||||||||||||
溶液配制表 | |||||||||||||||||||||||||||||||||||||||||
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