TRAM-34是中电导的钙激活的钾离子通道(KCa3.1),Kd为20 nM,不抑制细胞色素P450。
TRAM-34 is a selective and potent inhibitor of the intermediate-conductance Ca2+-activated K+ channel (IKCa1, KCa3.1) with Kd of 20 nM, 200- to 1500-fold selective over other ion channels, and does not block cytochrome P450. TRAM-34 has been shown to be an inhibitor of cloned and native IK1 channels in human T lymphocytes. These K+ channels have been implicated in over-proliferation of cells. Inhibition of IK1 channels has been demonstrated to modulate cell proliferation depending on the concentration of TRAM-34. Studies have shown that TRAM-34 may cause a halt in cell growth at the G0/G1 phase.
~10 μM
120 mg/kg/day皮下注射
动物 A (mg/kg) = 动物 B (mg/kg)×动物 B的Km系数/动物 A的Km系数 | |
例如,已知某工具药用于小鼠的剂量为88 mg/kg , 则用于大鼠的剂量换算方法:将88 mg/kg 乘以小鼠的Km系数(3),再除以大鼠的Km系数(6),得到该药物用于大鼠的等效剂量44 mg/kg。
[1] Wulff H, et al. Proc Natl Acad Sci U S A, 2000, 97(14), 8151-8156.
[2] Chandy, K.G., et al. 2004. Trends Pharmacol. Sci. 25: 280-289.
[3] Panyi, G., et al. 2006. Curr. Pharm. Des. 12: 2199-2220.
[4] Wang, Z.H., et al. 2007. Oncogene. 26: 5107-5114.
分子式 C22H17ClN2 |
分子量 344.84 |
CAS号 289905-88-0 |
储存方式 ﹣20 ℃冷藏长期储存。冰袋运输 |
溶剂(常温) |
DMSO 10 mg/mL at 40°C |
Water Insoluble |
Ethanol 6 mg/mL at 40°C |
体内溶解度
注:以上所有数据均来自公开文献,并不保证对所有实验均有效,数据仅供参考。
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