产品
编 号:F452477
分子式:C27H29N3O4
分子量:459.54
产品类型
结构图
CAS No: 763926-98-3
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产品详情
生物活性:
ORM-10962 is a potent, highly selective sodium-calcium exchanger (NCX) inhibitor, with IC50 values of 67 and 55 nM for the reverse and forward mode inhibition, respectively. ORM-10962 shows antiarrhythmic effect.
体内研究:
ORM-10962 (0.3 mg/kg,IV,一次) 预处理可显著延迟麻醉豚鼠心室期前收缩 (约 50%) 或室性心动过速 (约 30%) 的发生和复发。Animal Model:Male guinea-pigs (250-300 g)
Dosage:0.3 mg/kg
Administration:IV, 10 min before starting ouabain infusion
Result:Significantly delayed the development of ventricular extrasystoles (from 24±1.7 min in controls to 36.6±2.7 min in the presence of the drug) or ventricular tachycardia (from 31.8±1.8 min in controls to 40.8±2.1 min in the presence of the drug).
体外研究:
ORM-10962 (10 nM、100 nM 和 1 μM) 以浓度依赖性方式降低狗心室肌细胞中的 NCX 电流,在 -80 和 20 时的估计 IC50 值为 55 和 67 nM mV,分别为。