PF 915275是活性的,选择性 11β-hydroxysteroid dehydrogenase 抑制剂。
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] Fotsch and Wang (2008) Blockade of glucocorticoid excess at the tissue level: inhibitors of 11β-hydroxysteroid dehydrogenase type 1 as a therapy for type 2 diabetes. J.Med.Chem. 51 4851. PMID: 18652443.
[2] Courtney et al (2008) Modulation of 11β-hydroxysteroid dehydrogenase (11βHSD) activity biomarkers and pharmacokinetics of PF-00915275, a selective 11βHSD1 inhibitor. J.Clin.Endocrinol.Metab. 93 550. PMID: 17986636.
[3] Bhat et al (2008) Demonstration of proof of mechanism and pharmacokinetics and pharmacodynamic relationship with 4'-cyano-biphenyl-4-sulfonic acid (6-amino-pyridin-2-yl)-amide (PF-915275), an inhibitor of 11β-hydroxysteroid dehydrogenase type 1 in cynomolgus monkeys. J.Pharmacol.Exp.Ther. 324 299. PMID: 17921190.
分子式 C18H14N4O2S |
分子量 350.39 |
CAS号 857290-04-1 |
储存方式 ﹣20 ℃长期储存。冰袋运输 |
溶剂(常温) |
DMSO 100 mM |
Water |
Ethanol |
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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