Tadalafil is a potent and selective inhibitor of PDE5A (Phosphodiesterase-5, PDE5) with an IC50 value of 1.8 nM.
Tadalafil is a potent and selective inhibitor of PDE5A (Phosphodiesterase-5, PDE5) with an IC50 value of 1.8 nM. This compound prevents the breakdown of phosphodiesterases, many of which are used as secondary messengers. By preventing the breakdown of these messenger molecules, tadalafil can prolong signal transduction and amplify its effect.
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] Hak Joo Lee,et al. Tadalafil Integrates Nitric Oxide-Hydrogen Sulfide Signaling to Inhibit High Glucose-induced Matrix Protein Synthesis in Podocytes. J Biol Chem. 2015 May 8; 290(19): 12014–12026. Published online 2015 Mar 9. doi: 10.1074/jbc.M114.615377.
[2] Saisudha Koka,et al. Chronic inhibition of phosphodiesterase 5 with tadalafil attenuates mitochondrial dysfunction in type 2 diabetic hearts: potential role of NO/SIRT1/PGC-1α signaling. Am J Physiol Heart Circ Physiol. 2014 Jun 1; 306(11): H1558–H1568. Published online 2014 Apr 11. doi: 10.1152/ajpheart.00865.2013.
分子式 C22H19N3O4 |
分子量 389.4 |
CAS号 171596-29-5 |
储存方式 -20 ℃长期冷藏储存。冰袋运输 |
溶剂(常温) |
DMSO 78 mg/mL |
Water <1 mg/mL |
Ethanol <1 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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