Ambrisentan, a highly selective antagonist of the endothelin-1 type A receptor with IC50 of 18 nM, is indicated for the treatment of pulmonary arterial hypertension (PAH).
Ambrisentan, a highly selective antagonist of the endothelin-1 type A receptor with IC50 of 18 nM, is indicated for the treatment of pulmonary arterial hypertension (PAH).
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] Robyn J Barst. A review of pulmonary arterial hypertension: role of ambrisentan. Vasc Health Risk Manag. 2007 Feb; 3(1): 11–22.
[2] Eve-Irene Lepist,et al. Evaluation of the Endothelin Receptor Antagonists Ambrisentan, Bosentan, Macitentan, and Sitaxsentan as Hepatobiliary Transporter Inhibitors and Substrates in Sandwich-Cultured Human Hepatocytes. PLoS One. 2014; 9(1): e87548. Published online 2014 Jan 30. doi: 10.1371/journal.pone.0087548.
分子式 C22H22N2O4 |
分子量 378.42 |
CAS号 177036-94-1 |
储存方式 -20 ℃长期冷藏储存。冰袋运输 |
溶剂(常温) |
DMSO 75 mg/mL |
Water <1 mg/mL |
Ethanol 22 mg/mL |
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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